tag:blogger.com,1999:blog-18664220296599030412024-02-19T19:19:12.114+05:30Organometallic ChemistryCurrent Trends in Organometallic and Synthetic ChemistryUnknownnoreply@blogger.comBlogger5748125tag:blogger.com,1999:blog-1866422029659903041.post-37816930323215287952021-03-11T20:00:00.001+05:302021-03-11T20:00:44.643+05:30Development of a Highly Selective Plasmodium falciparum Proteasome Inhibitor with Anti‐malaria Activity in Humanized Mice<h1 class="citation__title"><a href="https://onlinelibrary.wiley.com/doi/10.1002/anie.202015845">Development of a Highly Selective <i>Plasmodium falciparum</i> Proteasome Inhibitor with Anti‐malaria Activity in Humanized Mice</a>
</h1>
<div class="accordion-tabbed__tab-mobile accordion__closed"><a aria-controls="a1" aria-haspopup="true" class="author-name accordion-tabbed__control" data-db-target-for="a1" data-id="a1" href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Zhan%2C+Wenhu" id="a1_Ctrl" role="button"><span>Dr. Wenhu Zhan</span></a><span class="author-name accordion-tabbed__control"><span>, </span></span><a aria-controls="a2" aria-haspopup="true" class="author-name accordion-tabbed__control" data-db-target-for="a2" data-id="a2" href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Zhang%2C+Hao" id="a2_Ctrl" role="button"><span>Dr. Hao Zhang</span></a><span class="author-name accordion-tabbed__control"><span>, </span></span><a aria-controls="a3" aria-haspopup="true" class="author-name accordion-tabbed__control" data-db-target-for="a3" data-id="a3" href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Ginn%2C+John" id="a3_Ctrl" role="button"><span>Dr. John Ginn</span></a><span class="author-name accordion-tabbed__control"><span>, </span></span><a aria-controls="a4" aria-haspopup="true" class="author-name accordion-tabbed__control" data-db-target-for="a4" data-id="a4" href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Leung%2C+Annie" id="a4_Ctrl" role="button"><span>Annie Leung</span></a><span class="author-name accordion-tabbed__control"><span>, </span></span><a aria-controls="a5" aria-haspopup="true" class="author-name accordion-tabbed__control" data-db-target-for="a5" data-id="a5" href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Liu%2C+Yi+J" id="a5_Ctrl" role="button"><span>Yi J. 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Tumwebaze</span></a><span class="author-name accordion-tabbed__control"><span>, </span></span><a aria-controls="a15" aria-haspopup="true" class="author-name accordion-tabbed__control" data-db-target-for="a15" data-id="a15" href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Lafuente-Monasterio%2C+Maria+Jose" id="a15_Ctrl" role="button"><span>Dr. Maria Jose Lafuente‐Monasterio</span></a><span class="author-name accordion-tabbed__control"><span>, </span></span><a aria-controls="a16" aria-haspopup="true" class="author-name accordion-tabbed__control" data-db-target-for="a16" data-id="a16" href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Martinez-Martinez%2C+Maria+Santos" id="a16_Ctrl" role="button"><span>Dr. Maria Santos Martinez‐Martinez</span></a><span class="author-name accordion-tabbed__control"><span>, </span></span><a aria-controls="a17" aria-haspopup="true" class="author-name accordion-tabbed__control" data-db-target-for="a17" data-id="a17" href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Vendome%2C+Jeremie" id="a17_Ctrl" role="button"><span>Dr. Jeremie Vendome</span></a><span class="author-name accordion-tabbed__control"><span>, </span></span><a aria-controls="a18" aria-haspopup="true" class="author-name accordion-tabbed__control" data-db-target-for="a18" data-id="a18" href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Beuming%2C+Thijs" id="a18_Ctrl" role="button"><span>Dr. Thijs Beumin</span></a><span class="author-name accordion-tabbed__control"><span>, </span></span><a aria-controls="a19" aria-haspopup="true" class="author-name accordion-tabbed__control" data-db-target-for="a19" data-id="a19" href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Sato%2C+Kenjiro" id="a19_Ctrl" role="button"><span>Dr. Kenjiro Sato</span></a><span class="author-name accordion-tabbed__control"><span>, </span></span><a aria-controls="a20" aria-haspopup="true" class="author-name accordion-tabbed__control" data-db-target-for="a20" data-id="a20" href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Aso%2C+Kazuyoshi" id="a20_Ctrl" role="button"><span>Dr. Kazuyoshi Aso</span></a><span class="author-name accordion-tabbed__control"><span>, </span></span><a aria-controls="a21" aria-haspopup="true" class="author-name accordion-tabbed__control" data-db-target-for="a21" data-id="a21" href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Rosenthal%2C+Philip+J" id="a21_Ctrl" role="button"><span>Prof. Dr. Philip J. Rosenthal</span></a><span class="author-name accordion-tabbed__control"><span>, </span></span><a aria-controls="a22" aria-haspopup="true" class="author-name accordion-tabbed__control" data-db-target-for="a22" data-id="a22" href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Cooper%2C+Roland+A" id="a22_Ctrl" role="button"><span>Prof. Dr. Roland A. Cooper</span></a><span class="author-name accordion-tabbed__control"><span>, </span></span><a aria-controls="a23" aria-haspopup="true" class="author-name accordion-tabbed__control" data-db-target-for="a23" data-id="a23" href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Meinke%2C+Peter+T" id="a23_Ctrl" role="button"><span>Dr. Peter T. Meinke</span></a><span class="author-name accordion-tabbed__control"><span>, </span></span><a aria-controls="a24" aria-haspopup="true" class="author-name accordion-tabbed__control" data-db-target-for="a24" data-id="a24" href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Nathan%2C+Carl+F" id="a24_Ctrl" role="button"><span>Prof. Dr. Carl F. Nathan</span></a><span class="author-name accordion-tabbed__control"><span>, </span></span><a aria-controls="a25" aria-haspopup="true" class="author-name accordion-tabbed__control" data-db-target-for="a25" data-id="a25" href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Kirkman%2C+Laura+A" id="a25_Ctrl" role="button"><span>Prof. Dr. Laura A. Kirkman</span></a><span class="author-name accordion-tabbed__control"><span>, </span></span><a aria-controls="a26" aria-haspopup="true" class="author-name accordion-tabbed__control" data-db-target-for="a26" data-id="a26" href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Lin%2C+Gang" id="a26_Ctrl" role="button"><span>Prof. Dr. Gang Lin</span></a><a aria-controls="a26" aria-haspopup="true" class="author-name accordion-tabbed__control" data-db-target-for="a26" data-id="a26" href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Lin%2C+Gang" id="a26_Ctrl" role="button"><span></span></a></div><p> </p><div class="separator" style="clear: both; text-align: center;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEh2hoprx75Y47qb44SE_J6Y5eXCSyzJCfe9hZoPvhvPpzwZJIs-aDYnfcMBjocjgvPDlRHjHoiC1t_s2xAnW5qR13HTWB4Sqk9NrklLrL5A84cd_Ks0Av26plLPwUfg2GOGTkKpl6pK369i/s700/1.webp" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="194" data-original-width="700" height="178" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEh2hoprx75Y47qb44SE_J6Y5eXCSyzJCfe9hZoPvhvPpzwZJIs-aDYnfcMBjocjgvPDlRHjHoiC1t_s2xAnW5qR13HTWB4Sqk9NrklLrL5A84cd_Ks0Av26plLPwUfg2GOGTkKpl6pK369i/w640-h178/1.webp" width="640" /> </a></div><div class="separator" style="clear: both; text-align: center;"> </div><div class="separator" style="clear: both; text-align: justify;"><i>Plasmodium falciparum</i> proteasome (Pf20S) inhibitors are active against <i>Plasmodium</i>
at multiple stages—erythrocytic, gametocyte, liver, and gamete
activation stages—indicating that selective Pf20S inhibitors possess the
potential to be therapeutic, prophylactic, and transmission‐blocking
antimalarials. Starting from a reported compound, we developed a
noncovalent, macrocyclic peptide inhibitor of the malarial proteasome
with high species selectivity and improved pharmacokinetic properties.
The compound demonstrates specific, time‐dependent inhibition of the β5
subunit of the <i>Pf20S</i>, kills artemisinin‐sensitive and artemisinin‐resistant <i>P. falciparum</i> isolates in vitro and reduces parasitemia in humanized, <i>P. falciparum</i>‐infected mice. <br /></div><div class="separator" style="clear: both; text-align: center;"> </div><br /><p></p>Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-57830030455589569422020-08-07T10:47:00.005+05:302020-08-07T10:49:11.139+05:30 A short de novo synthesis of nucleoside analogs<p> <a class="highwire-cite-linked-title" data-hide-link-title="0" data-icon-position="" href="https://science.sciencemag.org/content/369/6504/725" style="box-sizing: inherit; color: #37588a; font-family: "roboto condensed", "helvetica neue", helvetica, arial, sans-serif; font-size: 1.3125rem; text-decoration-line: none;">A short de novo synthesis of nucleoside analogs</a></p><p class="highwire-cite-authors byline" style="background-color: white; box-sizing: inherit; color: #666666; font-family: "roboto condensed", "helvetica neue", helvetica, arial, sans-serif; font-size: 0.75em; font-weight: 700; margin: 0px; text-transform: uppercase; width: 694.781px;">BY <span class="highwire-citation-authors" style="box-sizing: inherit;"><span class="highwire-citation-author first" data-delta="0" style="box-sizing: inherit;">MICHAEL MEANWELL</span>, <span class="highwire-citation-author" data-delta="1" style="box-sizing: inherit;">STEVEN M. SILVERMAN</span>, <span class="highwire-citation-author" data-delta="2" style="box-sizing: inherit;">JOHANNES LEHMANN</span>, <span class="highwire-citation-author" data-delta="3" style="box-sizing: inherit;">BHARANISHASHANK ADLURI</span>, <span class="highwire-citation-author" data-delta="4" style="box-sizing: inherit;">YANG WANG</span>, <span class="highwire-citation-author" data-delta="5" style="box-sizing: inherit;">RYAN COHEN</span>, <span class="highwire-citation-author" data-delta="6" style="box-sizing: inherit;">LOUIS-CHARLES CAMPEAU</span>, <span class="highwire-citation-author" data-delta="7" style="box-sizing: inherit;">ROBERT BRITTON</span></span></p><p class="highwire-cite-authors byline" style="background-color: white; box-sizing: inherit; color: #666666; font-family: "roboto condensed", "helvetica neue", helvetica, arial, sans-serif; font-size: 0.75em; font-weight: 700; margin: 0px; text-transform: uppercase; width: 694.781px;"><span class="highwire-citation-authors" style="box-sizing: inherit;"></span></p><div class="separator" style="clear: both;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEjBmNR1uTDQyene9BVeeDqvOO3o8bDgvl_A2jjkR47dCflCCeUG8M6xymXh-q8XfZv-AQdqXvBGxsnQctoI1NvMrDWrIzpFtflJGbgnPFkI53ouRl8LaRvReapA7sZnZqSxszZc7i3yAcbT/s979/S1.png" style="display: block; padding: 1em 0px; text-align: center;"><img border="0" data-original-height="626" data-original-width="979" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEjBmNR1uTDQyene9BVeeDqvOO3o8bDgvl_A2jjkR47dCflCCeUG8M6xymXh-q8XfZv-AQdqXvBGxsnQctoI1NvMrDWrIzpFtflJGbgnPFkI53ouRl8LaRvReapA7sZnZqSxszZc7i3yAcbT/s640/S1.png" width="640" /></a></div><p class="highwire-cite-authors byline" style="background-color: white; box-sizing: inherit; color: #666666; font-family: "roboto condensed", "helvetica neue", helvetica, arial, sans-serif; font-size: 0.75em; font-weight: 700; margin: 0px; text-align: left; text-transform: uppercase; width: 694.781px;"><span face="" style="background-color: #e6e6e6; color: #333333; font-family: roboto, "helvetica neue", helvetica, arial, sans-serif; font-size: 16px; font-weight: 400; text-align: justify; text-transform: none;">Nucleoside analogs are commonly used in the treatment of cancer and viral infections. Their syntheses benefit from decades of research but are often protracted, unamenable to diversification, and reliant on a limited pool of chiral carbohydrate starting materials. We present a process for rapidly constructing nucleoside analogs from simple achiral materials. Using only proline catalysis, heteroaryl-substituted acetaldehydes are fluorinated and then directly engaged in enantioselective aldol reactions in a one-pot reaction. A subsequent intramolecular fluoride displacement reaction provides a functionalized nucleoside analog. The versatility of this process is highlighted in multigram syntheses of </span><span class="sc" face="" style="background-color: #e6e6e6; box-sizing: inherit; color: #333333; font-family: roboto, "helvetica neue", helvetica, arial, sans-serif; font-size: 0.85em; font-variant-caps: small-caps; font-variant-east-asian: normal; font-variant-numeric: normal; font-weight: 400; text-align: justify;">D</span><span face="" style="background-color: #e6e6e6; color: #333333; font-family: roboto, "helvetica neue", helvetica, arial, sans-serif; font-size: 16px; font-weight: 400; text-align: justify; text-transform: none;">- or </span><span class="sc" face="" style="background-color: #e6e6e6; box-sizing: inherit; color: #333333; font-family: roboto, "helvetica neue", helvetica, arial, sans-serif; font-size: 0.85em; font-variant-caps: small-caps; font-variant-east-asian: normal; font-variant-numeric: normal; font-weight: 400; text-align: justify;">L</span><span face="" style="background-color: #e6e6e6; color: #333333; font-family: roboto, "helvetica neue", helvetica, arial, sans-serif; font-size: 16px; font-weight: 400; text-align: justify; text-transform: none;">-nucleoside analogs, locked nucleic acids, iminonucleosides, and C2′- and C4′-modified nucleoside analogs. This de novo synthesis creates opportunities for the preparation of diversity libraries and will support efforts in both drug discovery and development.</span></p>Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-52910808982282338682020-08-06T17:58:00.003+05:302020-08-06T17:58:47.854+05:30A photochemical dehydrogenative strategy for aniline synthesis<h3 class="mb10 extra-tight-line-height" itemprop="name headline" style="-webkit-font-smoothing: antialiased; background-color: white; color: #222222; font-family: Harding, Lora, Palatino, Times, "Times New Roman", serif; font-size: 2rem; line-height: 1.3; margin: 0px 0px 10px; padding: 0px;"><a data-track-action="view article" data-track-label="link" data-track="click" href="https://www.nature.com/articles/s41586-020-2539-7" itemprop="url" style="background-color: transparent; color: #006699; text-decoration-line: none; vertical-align: baseline;">A photochemical dehydrogenative strategy for aniline synthesis</a></h3><div class="mt4 mb10 serif text13 tighten-line-height text-gray suppress-bottom-margin hide-overflow inline" data-show-more-dest="web-sum" itemprop="description" style="background-color: white; color: #222222; display: inline; font-family: Harding, Palatino, serif; font-size: 1.3rem; line-height: 1.4; margin: 4px 0px 10px; overflow: hidden; padding: 0px;"><li itemprop="creator" itemscope="itemscope" itemtype="http://schema.org/Person" style="color: #666666; display: inline; font-family: -apple-system, BlinkMacSystemFont, "Segoe UI", Roboto, Oxygen-Sans, Ubuntu, Cantarell, "Helvetica Neue", sans-serif; font-size: 1.3rem;">Shashikant U. Dighe</li><li itemprop="creator" itemscope="itemscope" itemtype="http://schema.org/Person" style="color: #666666; display: inline; font-family: -apple-system, BlinkMacSystemFont, "Segoe UI", Roboto, Oxygen-Sans, Ubuntu, Cantarell, "Helvetica Neue", sans-serif; font-size: 1.3rem;">, <span itemprop="name">Fabio Juliá</span></li><li class="js-author-etal js-smaller-author-etal" itemprop="creator" itemscope="itemscope" itemtype="http://schema.org/Person" style="color: #666666; display: inline; font-family: -apple-system, BlinkMacSystemFont, "Segoe UI", Roboto, Oxygen-Sans, Ubuntu, Cantarell, "Helvetica Neue", sans-serif; font-size: 1.3rem; visibility: visible;">, <span itemprop="name">Alberto Luridiana</span></li><li class="js-author-etal js-smaller-author-etal" itemprop="creator" itemscope="itemscope" itemtype="http://schema.org/Person" style="color: #666666; display: inline; font-family: -apple-system, BlinkMacSystemFont, "Segoe UI", Roboto, Oxygen-Sans, Ubuntu, Cantarell, "Helvetica Neue", sans-serif; font-size: 1.3rem; visibility: visible;">, <span itemprop="name">James J. Douglas</span></li><li itemprop="creator" itemscope="itemscope" itemtype="http://schema.org/Person" style="color: #666666; display: inline; font-family: -apple-system, BlinkMacSystemFont, "Segoe UI", Roboto, Oxygen-Sans, Ubuntu, Cantarell, "Helvetica Neue", sans-serif; font-size: 1.3rem;"> & <span itemprop="name">Daniele Leonori</span></li></div><div><div class="mt4 mb10 serif text13 tighten-line-height text-gray suppress-bottom-margin hide-overflow inline" data-show-more-dest="web-sum" itemprop="description" style="background-color: white; color: #222222; display: inline; font-family: Harding, Palatino, serif; font-size: 1.3rem; line-height: 1.4; margin: 4px 0px 10px; overflow: hidden; padding: 0px;"><li itemprop="creator" itemscope="itemscope" itemtype="http://schema.org/Person" style="color: #666666; display: inline; font-family: -apple-system, BlinkMacSystemFont, "Segoe UI", Roboto, Oxygen-Sans, Ubuntu, Cantarell, "Helvetica Neue", sans-serif; font-size: 1.3rem;"><div><div class="mt4 mb10 serif text13 tighten-line-height text-gray suppress-bottom-margin hide-overflow inline" data-show-more-dest="web-sum" itemprop="description" style="background-color: white; color: #222222; display: inline; font-family: Harding, Palatino, serif; font-size: 1.3rem; line-height: 1.4; margin: 4px 0px 10px; overflow: hidden; padding: 0px;"></div></div></li><li itemprop="creator" itemscope="itemscope" itemtype="http://schema.org/Person" style="color: #666666; display: inline; font-family: -apple-system, BlinkMacSystemFont, "Segoe UI", Roboto, Oxygen-Sans, Ubuntu, Cantarell, "Helvetica Neue", sans-serif; font-size: 1.3rem;"><div class="separator" style="clear: both;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEgvZKUmhCMEOGVIrXrsH6HT0LCV6tbxvVoMTGcZVLF995TLpTXekzs_mpkuquGak-vJL3U_xDZoj4o43xoolb93KHclL4D5hUQI0aUnoW0yh_dT2QzvRISFzqs50qStG6RDPPQYYGJHeuGL/s2172/1.jpg" imageanchor="1" style="display: block; padding: 1em 0px; text-align: center;"><img border="0" data-original-height="666" data-original-width="2172" height="196" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEgvZKUmhCMEOGVIrXrsH6HT0LCV6tbxvVoMTGcZVLF995TLpTXekzs_mpkuquGak-vJL3U_xDZoj4o43xoolb93KHclL4D5hUQI0aUnoW0yh_dT2QzvRISFzqs50qStG6RDPPQYYGJHeuGL/w640-h196/1.jpg" width="640" /></a></div></li></div></div><li itemprop="creator" itemscope="itemscope" itemtype="http://schema.org/Person" style="color: #666666; display: inline; font-family: -apple-system, BlinkMacSystemFont, "Segoe UI", Roboto, Oxygen-Sans, Ubuntu, Cantarell, "Helvetica Neue", sans-serif; font-size: 1.3rem;"><div><div class="mt4 mb10 serif text13 tighten-line-height text-gray suppress-bottom-margin hide-overflow inline" data-show-more-dest="web-sum" itemprop="description" style="background-color: white; color: #222222; display: inline; font-family: Harding, Palatino, serif; font-size: 1.3rem; line-height: 1.4; margin: 4px 0px 10px; overflow: hidden; padding: 0px;"></div></div></li><li itemprop="creator" itemscope="itemscope" itemtype="http://schema.org/Person" style="color: #666666; display: inline; font-family: -apple-system, BlinkMacSystemFont, "Segoe UI", Roboto, Oxygen-Sans, Ubuntu, Cantarell, "Helvetica Neue", sans-serif; font-size: 1.3rem;"><span itemprop="name"><span style="color: #222222; font-family: Harding, Palatino, serif; font-size: 20.8px;">A dual cobalt and photocatalysis system provides a way to assemble anilines from cyclohexanones and amines by progressively dehydrating the intermediate imine.</span></span></li>Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-31989324072296363792020-08-06T17:51:00.005+05:302020-08-07T17:28:58.546+05:30Photoenzymatic enantioselective intermolecular radical hydroalkylation<h2 style="text-align: left;"><a href="https://www.blogger.com/#">Photoenzymatic enantioselective intermolecular radical hydroalkylation</a></h2>Xiaoqiang Huang , Binju Wang, Yajie Wang, Guangde Jiang, Jianqiang Feng & Huimin Zhao<div><div class="mt4 mb10 serif text13 tighten-line-height text-gray suppress-bottom-margin hide-overflow inline" data-show-more-dest="web-sum" style="display: inline; line-height: 1.4; margin: 4px 0px 10px; overflow: hidden; padding: 0px;"><li itemtype="http://schema.org/Person" style="background-color: white; color: #666666; display: inline; font-family: harding, palatino, serif; font-size: 1.3rem;"><div class="separator" style="clear: both;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhw5jn-aZOpxSZBuPh3v7ANX7gIB3kmhLLFx_87AYhNJJipfbF0Iha8AaEfRops6wxGCqMZTYpchjNeHVJ3YL-uAvwXOxZm0JA2RoxpOr7OtXXptUXRBZa-Q0XD0FmUui-zM_w1SWdRgAl2/s1250/1.jpg" style="display: block; padding: 1em 0px; text-align: center;"><img border="0" data-original-height="1250" data-original-width="976" height="640" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhw5jn-aZOpxSZBuPh3v7ANX7gIB3kmhLLFx_87AYhNJJipfbF0Iha8AaEfRops6wxGCqMZTYpchjNeHVJ3YL-uAvwXOxZm0JA2RoxpOr7OtXXptUXRBZa-Q0XD0FmUui-zM_w1SWdRgAl2/s640/1.jpg" /></a></div></li><li itemtype="http://schema.org/Person" style="background-color: white; color: #666666; display: inline; font-family: harding, palatino, serif; font-size: 1.3rem;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhw5jn-aZOpxSZBuPh3v7ANX7gIB3kmhLLFx_87AYhNJJipfbF0Iha8AaEfRops6wxGCqMZTYpchjNeHVJ3YL-uAvwXOxZm0JA2RoxpOr7OtXXptUXRBZa-Q0XD0FmUui-zM_w1SWdRgAl2/s1250/1.jpg" style="display: block; padding: 1em 0px; text-align: center;"><br /></a></li>A transformation in which an ‘ene’ reductase catalyses the visible-light-induced intermolecular radical hydroalkylation of alkenes gives carbonyl compounds with a remote stereocentre in high yield and enantioselectivity.</div></div>Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-11250626013467806852020-08-06T17:45:00.001+05:302020-08-06T17:45:07.331+05:30Chemo‐ and Enantioselective Oxidative α‐Azidation of Carbonyl Compounds<a class="issue-item__title visitable" href="https://onlinelibrary.wiley.com/doi/10.1002/anie.202007552" style="background-color: white; box-sizing: border-box; clear: both; color: #61165e; cursor: pointer; display: block; font-family: "Open Sans", icomoon, sans-serif; font-size: 14px; line-height: 22px; margin: 10px 0px; outline: 0px; text-decoration-line: none;"><h2 style="box-sizing: border-box; font-size: 16px; margin: 0px;">Chemo‐ and Enantioselective Oxidative α‐Azidation of Carbonyl Compounds</h2></a><ul class="rlist--inline loa comma loa-authors-trunc" style="background-color: white; box-sizing: border-box; color: #767676; float: none; font-family: "Open Sans", icomoon, sans-serif; font-size: 14px; line-height: 22px; list-style: none; margin: 10px 0px; padding: 0px; position: static;"><li style="box-sizing: border-box; display: inline-block;"><a href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Uyanik%2C+Muhammet" style="background-color: transparent; box-sizing: border-box; color: #767676; cursor: pointer; text-decoration-line: none;" title="Prof. Dr. Muhammet Uyanik">Prof. Dr. Muhammet Uyanik</a></li> <li style="box-sizing: border-box; display: inline-block;"><a href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Sahara%2C+Naoto" style="background-color: transparent; box-sizing: border-box; color: #767676; cursor: pointer; text-decoration-line: none;" title="Dr. Naoto Sahara">Dr. Naoto Sahara</a></li> <li style="box-sizing: border-box; display: inline-block;"><a href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Tsukahara%2C+Mayuko" style="background-color: transparent; box-sizing: border-box; color: #767676; cursor: pointer; text-decoration-line: none;" title="Mayuko Tsukahara">Mayuko Tsukahara</a></li> <li style="box-sizing: border-box; display: inline-block;"><a href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Hattori%2C+Yuhei" style="background-color: transparent; box-sizing: border-box; color: #767676; cursor: pointer; text-decoration-line: none;" title="Yuhei Hattori">Yuhei Hattori</a></li> <li style="box-sizing: border-box; display: inline-block;"><a href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Ishihara%2C+Kazuaki" style="background-color: transparent; box-sizing: border-box; color: #767676; cursor: pointer; text-decoration-line: none;" title="Prof. Dr. Kazuaki Ishihara">Prof. Dr. Kazuaki Ishihara</a></li><li style="box-sizing: border-box; display: inline-block;"></li><li><br /><div class="separator" style="clear: both;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEiqLb96RiQuvH6gTDc1oHEm_y2CZkNF5sXKZtKclssolNGJ1iu8_D7jT8ZsQ8A0yUnOl0u8bRk-Q4SZLkY6Avi2g_PqfHVivDhPKMerYc51cc22EQSmYPlDRGwgU2wjR2S-NDBZuaN0Yqru/s430/1.jpg" imageanchor="1" style="display: block; padding: 1em 0px; text-align: center;"><img border="0" data-original-height="328" data-original-width="430" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEiqLb96RiQuvH6gTDc1oHEm_y2CZkNF5sXKZtKclssolNGJ1iu8_D7jT8ZsQ8A0yUnOl0u8bRk-Q4SZLkY6Avi2g_PqfHVivDhPKMerYc51cc22EQSmYPlDRGwgU2wjR2S-NDBZuaN0Yqru/s0/1.jpg" /></a></div></li></ul><div style="text-align: justify;"><span style="background-color: white; color: #1c1d1e; font-family: "Open Sans", icomoon, sans-serif; font-size: 14px; text-align: start;">High‐performance hypoiodite catalysis was developed for the chemoselective oxidative or decarboxylative oxidative α‐azidation of 1,3‐dicarbonyl compounds (see scheme). By this method, the late‐stage azidation of complex molecules with NaN</span><span style="background-color: white; bottom: -0.25em; box-sizing: border-box; color: #1c1d1e; font-family: "Open Sans", icomoon, sans-serif; font-size: 10.5px; line-height: 0; position: relative; text-align: start; vertical-align: baseline;">3</span><span style="background-color: white; color: #1c1d1e; font-family: "Open Sans", icomoon, sans-serif; font-size: 14px; text-align: start;"> and hydrogen peroxide as the azide source and oxidant, respectively, was possible under extremely mild conditions.</span></div>Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-18117010549148911942020-08-05T16:40:00.007+05:302020-08-05T16:40:59.101+05:30Palladium(II)‐Catalyzed Enantioselective Azidation of Unactivated Alkenes<a class="issue-item__title visitable" href="https://onlinelibrary.wiley.com/doi/10.1002/anie.202006757" style="background-color: white; box-sizing: border-box; clear: both; color: #61165e; cursor: pointer; display: block; font-family: "Open Sans", icomoon, sans-serif; font-size: 14px; line-height: 22px; margin: 10px 0px; outline: 0px; text-decoration-line: none;"><h2 style="box-sizing: border-box; font-size: 16px; margin: 0px;">Palladium(II)‐Catalyzed Enantioselective Azidation of Unactivated Alkenes</h2></a><ul class="rlist--inline loa comma loa-authors-trunc" style="background-color: white; box-sizing: border-box; color: #767676; float: none; font-family: "Open Sans", icomoon, sans-serif; font-size: 14px; line-height: 22px; list-style: none; margin: 10px 0px; padding: 0px; position: static;"><li style="box-sizing: border-box; display: inline-block;"><a href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Li%2C+Xiaonan" style="background-color: transparent; box-sizing: border-box; color: #767676; cursor: pointer; text-decoration-line: none;" title="Xiaonan Li">Xiaonan Li</a></li> <li style="box-sizing: border-box; display: inline-block;"><a href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Qi%2C+Xiaoxu" style="background-color: transparent; box-sizing: border-box; color: #767676; cursor: pointer; text-decoration-line: none;" title="Dr. Xiaoxu Qi">Dr. Xiaoxu Qi</a></li> <li style="box-sizing: border-box; display: inline-block;"><a href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Hou%2C+Chuanqi" style="background-color: transparent; box-sizing: border-box; color: #767676; cursor: pointer; text-decoration-line: none;" title="Chuanqi Hou">Chuanqi Hou</a></li> <li style="box-sizing: border-box; display: inline-block;"><a href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Chen%2C+Pinhong" style="background-color: transparent; box-sizing: border-box; color: #767676; cursor: pointer; text-decoration-line: none;" title="Dr. Pinhong Chen">Dr. Pinhong Chen</a></li> <li style="box-sizing: border-box; display: inline-block;"><a href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Liu%2C+Guosheng" style="background-color: transparent; box-sizing: border-box; color: #767676; cursor: pointer; text-decoration-line: none;" title="Prof. Dr. Guosheng Liu">Prof. Dr. Guosheng Liu</a></li><li style="box-sizing: border-box; display: inline-block;"></li><li><br /><div class="separator" style="clear: both; text-align: center;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhlFFYESsibZ7yFtbEx1BATNgybN_PQgGiqMNp6eYXHMRcHyAYsJ-OiPom6IvYIqnnHCCUr2K6VAx7OyKqo-dml6JfuZJ9wCpiR2s-R2fEejC4P9LXBzFQMhEUfyDEl_8gI21YHxck_1lAx/s896/1.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="164" data-original-width="896" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhlFFYESsibZ7yFtbEx1BATNgybN_PQgGiqMNp6eYXHMRcHyAYsJ-OiPom6IvYIqnnHCCUr2K6VAx7OyKqo-dml6JfuZJ9wCpiR2s-R2fEejC4P9LXBzFQMhEUfyDEl_8gI21YHxck_1lAx/s640/1.jpg" width="640" /></a></div></li></ul><div style="text-align: justify;"><span style="background-color: white; box-sizing: border-box; color: #1c1d1e; font-family: "Open Sans", icomoon, sans-serif; font-size: 14px; font-weight: bolder; text-align: start;">A Pd‐catalyzed </span><span style="background-color: white; color: #1c1d1e; font-family: "Open Sans", icomoon, sans-serif; font-size: 14px; text-align: start;">enantioselective intramolecular aminoazidation of unactivated alkenes using readily accessible 1‐azido‐1,2‐benziodoxol‐3(1</span><i style="background-color: white; box-sizing: border-box; color: #1c1d1e; font-family: "Open Sans", icomoon, sans-serif; font-size: 14px; text-align: start;">H </i><span style="background-color: white; color: #1c1d1e; font-family: "Open Sans", icomoon, sans-serif; font-size: 14px; text-align: start;">)‐one (ABX) as an azidating agent was established. This reaction affords a wide variety of structurally diverse 3‐N</span><span style="background-color: white; bottom: -0.25em; box-sizing: border-box; color: #1c1d1e; font-family: "Open Sans", icomoon, sans-serif; font-size: 10.5px; line-height: 0; position: relative; text-align: start; vertical-align: baseline;">3</span><span style="background-color: white; color: #1c1d1e; font-family: "Open Sans", icomoon, sans-serif; font-size: 14px; text-align: start;">‐substituted piperidines in good yields with excellent enantioselectivity, proceeds under mild reaction conditions, and features good functional‐group compatibility.</span></div>Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-85433966260869452012020-08-05T16:39:00.001+05:302020-08-05T16:39:05.998+05:30Synthesis, Characterization, and Reactivity of a Hypervalent‐Iodine‐Based Nitrooxylating Reagent<a class="issue-item__title visitable" href="https://onlinelibrary.wiley.com/doi/10.1002/anie.202005720" style="background-color: white; box-sizing: border-box; clear: both; color: #61165e; cursor: pointer; display: block; font-family: "Open Sans", icomoon, sans-serif; font-size: 14px; line-height: 22px; margin: 10px 0px; outline: 0px; text-decoration-line: none;"><h2 style="box-sizing: border-box; font-size: 16px; margin: 0px;">Synthesis, Characterization, and Reactivity of a Hypervalent‐Iodine‐Based Nitrooxylating Reagent</h2></a><ul class="rlist--inline loa comma loa-authors-trunc" style="background-color: white; box-sizing: border-box; color: #767676; float: none; font-family: "Open Sans", icomoon, sans-serif; font-size: 14px; line-height: 22px; list-style: none; margin: 10px 0px; padding: 0px; position: static;"><li style="box-sizing: border-box; display: inline-block;"><a href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Calvo%2C+Roxan" style="background-color: transparent; box-sizing: border-box; color: #767676; cursor: pointer; text-decoration-line: none;" title="Roxan Calvo">Roxan Calvo</a></li> <li style="box-sizing: border-box; display: inline-block;"><a href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=le+Tellier%2C+Antoine" style="background-color: transparent; box-sizing: border-box; color: #767676; cursor: pointer; text-decoration-line: none;" title="Antoine Le Tellier">Antoine Le Tellier</a></li> <li style="box-sizing: border-box; display: inline-block;"><a href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Nauser%2C+Thomas" style="background-color: transparent; box-sizing: border-box; color: #767676; cursor: pointer; text-decoration-line: none;" title="Dr. Thomas Nauser">Dr. Thomas Nauser</a></li> <li style="box-sizing: border-box; display: inline-block;"><a href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Rombach%2C+David" style="background-color: transparent; box-sizing: border-box; color: #767676; cursor: pointer; text-decoration-line: none;" title="Dr. David Rombach">Dr. David Rombach</a></li> <li style="box-sizing: border-box; display: inline-block;"><a href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Nater%2C+Darryl" style="background-color: transparent; box-sizing: border-box; color: #767676; cursor: pointer; text-decoration-line: none;" title="Darryl Nater">Darryl Nater</a></li> <li style="box-sizing: border-box; display: inline-block;"><a href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Katayev%2C+Dmitry" style="background-color: transparent; box-sizing: border-box; color: #767676; cursor: pointer; text-decoration-line: none;" title="Dr. Dmitry Katayev">Dr. Dmitry Katayev</a></li><li style="box-sizing: border-box; display: inline-block;"></li><li><br /><div class="separator" style="clear: both; text-align: center;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEjSk6G6N7pQmreJkeedowNsPj-P-rpSTpMFYWE3xqq1Fj8xxOJjir-hilnq5K6pDbxzVbKY4U2MTxXs-TXLeP-S8nqV2cHIzrtc65s_r_YQmxODdYX1jPHEeUp0MYVPotnYL5xBbLnuaRS3/s860/1.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="162" data-original-width="860" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEjSk6G6N7pQmreJkeedowNsPj-P-rpSTpMFYWE3xqq1Fj8xxOJjir-hilnq5K6pDbxzVbKY4U2MTxXs-TXLeP-S8nqV2cHIzrtc65s_r_YQmxODdYX1jPHEeUp0MYVPotnYL5xBbLnuaRS3/s640/1.jpg" width="640" /></a></div></li></ul><div style="text-align: justify;"><span style="background-color: white; box-sizing: border-box; color: #1c1d1e; font-family: "Open Sans", icomoon, sans-serif; font-size: 14px; font-weight: bolder; text-align: start;">Organic nitrate esters </span><span style="background-color: white; color: #1c1d1e; font-family: "Open Sans", icomoon, sans-serif; font-size: 14px; text-align: start;">were synthesized through the use of a hypervalent‐iodine‐based nitrooxylating reagent. Its versatile reactivity under various reaction conditions is demonstrated in the synthesis of nitrooxylated β‐keto esters, 1,3‐diketones, malonates, and oxindoles under mild conditions.</span></div>Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-21547671500900356402020-08-05T16:37:00.000+05:302020-08-05T16:37:02.364+05:30Cobalt‐Catalyzed C8‐Dienylation of Quinoline‐N‐Oxides<a class="issue-item__title visitable" href="https://onlinelibrary.wiley.com/doi/10.1002/anie.202003216" style="background-color: white; box-sizing: border-box; clear: both; color: #61165e; cursor: pointer; display: block; font-family: "Open Sans", icomoon, sans-serif; font-size: 14px; line-height: 22px; margin: 10px 0px; outline: 0px; text-decoration-line: none;"><h2 style="box-sizing: border-box; font-size: 16px; margin: 0px;">Cobalt‐Catalyzed C8‐Dienylation of Quinoline‐<i style="box-sizing: border-box;">N</i>‐Oxides</h2></a><ul class="rlist--inline loa comma loa-authors-trunc" style="background-color: white; box-sizing: border-box; color: #767676; float: none; font-family: "Open Sans", icomoon, sans-serif; font-size: 14px; line-height: 22px; list-style: none; margin: 10px 0px; padding: 0px; position: static; text-align: left;"><li style="box-sizing: border-box; display: inline-block;"><a href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Shukla%2C+Rahul+K" style="background-color: transparent; box-sizing: border-box; color: #767676; cursor: pointer; text-decoration-line: none;" title="Rahul K. Shukla">Rahul K. Shukla</a></li> <li style="box-sizing: border-box; display: inline-block;"><a href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Nair%2C+Akshay+M" style="background-color: transparent; box-sizing: border-box; color: #767676; cursor: pointer; text-decoration-line: none;" title="Akshay M. Nair">Akshay M. Nair</a></li> <li style="box-sizing: border-box; display: inline-block;"><a href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Khan%2C+Salman" style="background-color: transparent; box-sizing: border-box; color: #767676; cursor: pointer; text-decoration-line: none;" title="Salman Khan">Salman Khan</a></li> <li style="box-sizing: border-box; display: inline-block;"><a href="https://onlinelibrary.wiley.com/action/doSearch?ContribAuthorStored=Volla%2C+Chandra+M+R" style="background-color: transparent; box-sizing: border-box; color: #767676; cursor: pointer; text-decoration-line: none;" title="Prof. Chandra M. R. Volla">Prof. Chandra M. R. Volla</a></li><li style="box-sizing: border-box; display: inline-block;"></li><li><br /><div class="separator" style="clear: both; text-align: center;"><a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEjgXA99bAc6uyZAJQ_8Og423LjB8xwr5IKY8T7rYcj7PU77Awi-mibwcpLWVl9NtLpuCzE5niRIsesJo1n8UWM_F5iuCJTTxbayucuoakwhl2Whs8Rr4hGYsnbwEojislhCcukhLwOpcX7u/s686/1.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="188" data-original-width="686" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEjgXA99bAc6uyZAJQ_8Og423LjB8xwr5IKY8T7rYcj7PU77Awi-mibwcpLWVl9NtLpuCzE5niRIsesJo1n8UWM_F5iuCJTTxbayucuoakwhl2Whs8Rr4hGYsnbwEojislhCcukhLwOpcX7u/s640/1.jpg" width="640" /></a></div></li><li style="text-align: justify;"><font color="#767676" face="Open Sans, icomoon, sans-serif"><span style="font-size: 14px;"><span style="box-sizing: border-box; color: #1c1d1e; font-weight: bolder;">Co<span style="box-sizing: border-box; font-size: 10.5px; line-height: 0; position: relative; top: -0.5em; vertical-align: baseline;">III</span>‐catalyzed </span><span style="color: #1c1d1e;">site‐selective C8−H activation of quinoline </span><i style="box-sizing: border-box; color: #1c1d1e;">N</i><span style="color: #1c1d1e;">‐oxides is demonstrated, engaging allenes as dienylation partners under relatively mild reaction conditions. The combination of a carbonate leaving group on the allene and 30 mol % of a NaF additive was found to be crucial for the dienylation reaction with a broad range of quinoline </span><i style="box-sizing: border-box; color: #1c1d1e;">N</i><span style="color: #1c1d1e;">‐oxides and allenes, including late‐stage functionalizations. Mechanistic studies provide key insights into the reaction mechanism.</span></span></font></li></ul>Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-72570762089824821242019-01-18T17:39:00.000+05:302019-01-18T17:39:09.512+05:30Review:The importance of synthetic chemistry in the pharmaceutical industry<div dir="ltr" style="text-align: left;" trbidi="on">
Science<br />
<h3 class="highwire-cite-title-wrapper media__headline" style="background-color: white; box-sizing: inherit; color: #333333; font-family: "Roboto Condensed", "Helvetica Neue", Helvetica, Arial, sans-serif; font-size: 1.3125rem; line-height: 1.2; margin-bottom: 7.5px; margin-top: 0px; padding-top: 0px;">
<div class="highwire-cite-title media__headline__title" style="box-sizing: inherit;">
<a href="http://science.sciencemag.org/content/363/6424/eaat0805" target="_blank">The importance of synthetic chemistry in the pharmaceutical industry</a></div>
</h3>
<div class="highwire-cite-authors byline" style="background-color: white; box-sizing: inherit; color: #666666; font-family: "Roboto Condensed", "Helvetica Neue", Helvetica, Arial, sans-serif; font-size: 0.75em; font-weight: bold; text-transform: uppercase; width: 694.781px;">
BY <span class="highwire-citation-authors" style="box-sizing: inherit;"><span class="highwire-citation-author first" data-delta="0" style="box-sizing: inherit;">KEVIN R. CAMPOS</span>, <span class="highwire-citation-author" data-delta="1" style="box-sizing: inherit;">PAUL J. COLEMAN</span>, <span class="highwire-citation-author" data-delta="2" style="box-sizing: inherit;">JUAN C. ALVAREZ</span>, <span class="highwire-citation-author" data-delta="3" style="box-sizing: inherit;">SPENCER D. DREHER</span>, <span class="highwire-citation-author" data-delta="4" style="box-sizing: inherit;">ROBERT M. GARBACCIO</span>, <span class="highwire-citation-author" data-delta="5" style="box-sizing: inherit;">NICHOLAS K. TERRETT</span>, <span class="highwire-citation-author" data-delta="6" style="box-sizing: inherit;">RICHARD D. TILLYER</span>, <span class="highwire-citation-author" data-delta="7" style="box-sizing: inherit;">MATTHEW D. TRUPPO</span>, <span class="highwire-citation-author" data-delta="8" style="box-sizing: inherit;">EMMA R. PARMEE</span></span></div>
<div class="highwire-cite-authors byline" style="background-color: white; box-sizing: inherit; color: #666666; font-family: "Roboto Condensed", "Helvetica Neue", Helvetica, Arial, sans-serif; font-size: 0.75em; font-weight: bold; text-transform: uppercase; width: 694.781px;">
<span class="highwire-citation-authors" style="box-sizing: inherit;"><span class="highwire-citation-author" data-delta="8" style="box-sizing: inherit;"><br /></span></span></div>
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<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhtj6pjlJYSCX3GyGRCDLgwObaHgHUi12vI-OulVjNBsb_UVk-zlkd-Cm87TTEyQux0OSYYqMZfV_XAkGDmZhHjL7EGWi2peu2Enm3MEukVbeuZbJS2uU0UpdLUek6x52w_wItDfpXI9UzX/s1600/1.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="615" data-original-width="1280" height="305" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhtj6pjlJYSCX3GyGRCDLgwObaHgHUi12vI-OulVjNBsb_UVk-zlkd-Cm87TTEyQux0OSYYqMZfV_XAkGDmZhHjL7EGWi2peu2Enm3MEukVbeuZbJS2uU0UpdLUek6x52w_wItDfpXI9UzX/s640/1.jpg" width="640" /></a></div>
<div class="highwire-cite-authors byline" style="background-color: white; box-sizing: inherit; color: #666666; font-family: "Roboto Condensed", "Helvetica Neue", Helvetica, Arial, sans-serif; font-size: 0.75em; font-weight: bold; text-align: justify; text-transform: uppercase; width: 694.781px;">
<span class="highwire-citation-authors" style="box-sizing: inherit;"><span class="highwire-citation-author" data-delta="8" style="box-sizing: inherit;"><span style="background-color: #e6e6e6; color: #333333; font-family: Roboto, "Helvetica Neue", Helvetica, Arial, sans-serif; font-size: 16px; font-weight: 400; text-transform: none;">Chemical synthesis plays a key role in pharmaceutical research and development. Campos </span><em style="background-color: #e6e6e6; box-sizing: inherit; color: #333333; font-family: Roboto, "Helvetica Neue", Helvetica, Arial, sans-serif; font-size: 16px; font-weight: 400; text-transform: none;">et al.</em><span style="background-color: #e6e6e6; color: #333333; font-family: Roboto, "Helvetica Neue", Helvetica, Arial, sans-serif; font-size: 16px; font-weight: 400; text-transform: none;"> review some of the advantages that have come from recent innovations in synthetic methods. In particular, they highlight small-molecule catalysts stimulated by visible light, enzymes engineered for versatility beyond their intrinsic function, and bio-orthogonal reactions to selectively modify proteins for conjugation. High-throughput techniques are also poised to accelerate methods optimization from small-scale discovery to large-scale production, and complementary machine-learning approaches are just coming into focus.</span></span></span></div>
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Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-34914408284359559822019-01-18T17:36:00.001+05:302019-01-18T17:36:22.699+05:30Concise total syntheses of (–)-jorunnamycin A and (–)-jorumycin enabled by asymmetric catalysis<div dir="ltr" style="text-align: left;" trbidi="on">
Science<br />
<br />
<h3 class="highwire-cite-title-wrapper media__headline" style="background-color: white; box-sizing: inherit; color: #333333; font-family: "Roboto Condensed", "Helvetica Neue", Helvetica, Arial, sans-serif; font-size: 1.3125rem; line-height: 1.2; margin-bottom: 7.5px; margin-top: 0px; padding-top: 0px;">
<div class="highwire-cite-title media__headline__title" style="box-sizing: inherit;">
<a href="http://science.sciencemag.org/content/363/6424/270" target="_blank">Concise total syntheses of (–)-jorunnamycin A and (–)-jorumycin enabled by asymmetric catalysis</a></div>
</h3>
<div class="highwire-cite-authors byline" style="background-color: white; box-sizing: inherit; color: #666666; font-family: "Roboto Condensed", "Helvetica Neue", Helvetica, Arial, sans-serif; font-size: 0.75em; font-weight: bold; text-transform: uppercase; width: 694.781px;">
BY <span class="highwire-citation-authors" style="box-sizing: inherit;"><span class="highwire-citation-author first" data-delta="0" style="box-sizing: inherit;">ERIC R. WELIN</span>, <span class="highwire-citation-author" data-delta="1" style="box-sizing: inherit;">AURAPAT NGAMNITHIPORN</span>, <span class="highwire-citation-author" data-delta="2" style="box-sizing: inherit;">MAX KLATTE</span>, <span class="highwire-citation-author" data-delta="3" style="box-sizing: inherit;">GUILLAUME LAPOINTE</span>, <span class="highwire-citation-author" data-delta="4" style="box-sizing: inherit;">GERIT M. POTOTSCHNIG</span>, <span class="highwire-citation-author" data-delta="5" style="box-sizing: inherit;">MARTINA S. J. MCDERMOTT</span>, <span class="highwire-citation-author" data-delta="6" style="box-sizing: inherit;">DYLAN CONKLIN</span>, <span class="highwire-citation-author" data-delta="7" style="box-sizing: inherit;">CHRISTOPHER D. GILMORE</span>, <span class="highwire-citation-author" data-delta="8" style="box-sizing: inherit;">PAMELA M. TADROSS</span>, <span class="highwire-citation-author" data-delta="9" style="box-sizing: inherit;">CHRISTOPHER K. HALEY</span>, <span class="highwire-citation-author" data-delta="10" style="box-sizing: inherit;">KENJI NEGORO</span>, <span class="highwire-citation-author" data-delta="11" style="box-sizing: inherit;">EMIL GLIBSTRUP</span>, <span class="highwire-citation-author" data-delta="12" style="box-sizing: inherit;">CHRISTIAN U. GRÜNANGER</span>, <span class="highwire-citation-author" data-delta="13" style="box-sizing: inherit;">KEVIN M. ALLAN</span>, <span class="highwire-citation-author" data-delta="14" style="box-sizing: inherit;">SCOTT C. VIRGIL</span>, <span class="highwire-citation-author" data-delta="15" style="box-sizing: inherit;">DENNIS J. SLAMON</span>, <span class="highwire-citation-author" data-delta="16" style="box-sizing: inherit;">BRIAN M. STOLTZ</span></span></div>
<div class="highwire-cite-metadata byline" style="background-color: white; box-sizing: inherit; color: #666666; font-family: "Roboto Condensed", "Helvetica Neue", Helvetica, Arial, sans-serif; font-size: 0.75em; font-weight: bold; text-transform: uppercase; width: 694.781px;">
<em style="box-sizing: inherit;">SCIENCE</em><time style="border-left: 1px solid rgb(102, 102, 102); box-sizing: inherit; margin-left: 7.5px; padding-left: 7.5px; white-space: nowrap;">18 JAN 2019</time> : 270-275 <span class="highwire-citation-access highwire-citation-access-check" data-atom-uri="/sci/363/6424/270.atom" data-pisa-id="sci;science.aav3421" data-request-view="full" style="border-left: 1px solid rgb(102, 102, 102); box-sizing: inherit; margin-left: 7.5px; padding-left: 7.5px; white-space: nowrap;"><span aria-hidden="true" class="highwire-access-icon highwire-access-icon-user-access user-access fa fa-unlock-alt" style="-webkit-font-smoothing: antialiased; box-sizing: inherit; display: inline-block; font-family: FontAwesome; font-size: inherit; font-stretch: normal; font-variant-east-asian: normal; font-variant-numeric: normal; font-weight: normal; line-height: 1; text-rendering: auto; transform: translate(0px, 0px);" title="Full Access"></span><span class="element-invisible highwire-access-icon highwire-access-icon-user-access" style="border: 0px !important; box-sizing: inherit; clip: rect(1px, 1px, 1px, 1px); height: 0px !important; margin: 0px !important; max-height: 1px !important; max-width: 1px !important; overflow: hidden; padding: 0px !important; position: absolute !important; width: 0px !important;"></span></span></div>
<div class="highwire-cite-snippet media__deck" style="background-color: white; box-sizing: inherit; color: #333333; font-family: Roboto, "Helvetica Neue", Helvetica, Arial, sans-serif; font-size: 0.875rem; margin-top: 15px;">
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<div class="section precis" id="abstract-2" style="box-sizing: inherit; transition: background-color 1s ease-in-out 1s;" xmlns:xhtml="http://www.w3.org/1999/xhtml" xmlns="http://www.w3.org/1999/xhtml">
<div id="p-4" style="box-sizing: inherit; margin-bottom: 15px; margin-top: 15px; transition: background-color 1s ease-in-out 1s; width: 694.781px;">
A route to two marine natural products distinct from the biosynthesis enables structural diversification for drug discovery.</div>
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<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEg76i9co8y7IezsyvPPUe2hvYXtjUG9yLwvYc1iPJFsV-fmkhCxahiBrO8CoNQVsK_qw9WDEb8txianBJ71K5pcyL6w8S6hx9mvrNyKr_wZKodYjUu9PiOxxEqww_buOXYXJAdGV8CDhJKg/s1600/1.png" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="537" data-original-width="1278" height="268" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEg76i9co8y7IezsyvPPUe2hvYXtjUG9yLwvYc1iPJFsV-fmkhCxahiBrO8CoNQVsK_qw9WDEb8txianBJ71K5pcyL6w8S6hx9mvrNyKr_wZKodYjUu9PiOxxEqww_buOXYXJAdGV8CDhJKg/s640/1.png" width="640" /></a></div>
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<span style="background-color: #e6e6e6; font-size: 16px;">Jorumycin is a structurally complex, pentacyclic organic compound produced by a marine mollusk. The success of a similar compound, trabectedin, in treating certain types of cancer has focused attention on exploring jorumycin's pharmaceutical properties. Welin </span><em style="background-color: #e6e6e6; box-sizing: inherit; font-size: 16px;">et al.</em><span style="background-color: #e6e6e6; font-size: 16px;">developed a succinct route to synthesizing jorumycin and the closely related jorunnamycin A that deliberately diverges from the putative biosynthetic pathway underlying prior chemical syntheses. This route, which hinges on a carefully optimized asymmetric catalytic hydrogenation, can be easily modified to introduce unnatural structural diversity for functional optimization in further drug discovery research.</span></div>
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Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-21955980923551316892019-01-10T22:19:00.001+05:302019-01-10T22:19:07.773+05:30Divergent Synthesis of Natural Derivatives of (+)‐Saxitoxin Including 11‐Saxitoxinethanoic Acid<div dir="ltr" style="text-align: left;" trbidi="on">
Angewchem<br />
<a href="https://onlinelibrary.wiley.com/doi/10.1002/anie.201811717">Divergent Synthesis of Natural Derivatives of (+)‐Saxitoxin Including 11‐Saxitoxinethanoic Acid</a><br /> Dr. James R. Walker, Dr. Jeffrey E. Merit, Dr. Rhiannon Thomas‐Tran, Doris T. Y. Tang, Prof. J. Du Bois<br />
<div class="separator" style="clear: both; text-align: center;">
<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEjefte0AafDu56GQCt5Uogx-7zA3IrLnxZRzcWZQU2Us3wygm9H6tT4lzmKewHazAVovzdVEH7c-c-QuAgQ7ATUuIdesnsIwymplLOudr3qQ91cHLUeUKlhiNcxscBpuGr20aZZj6cLQgoF/s1600/1.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="138" data-original-width="860" height="102" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEjefte0AafDu56GQCt5Uogx-7zA3IrLnxZRzcWZQU2Us3wygm9H6tT4lzmKewHazAVovzdVEH7c-c-QuAgQ7ATUuIdesnsIwymplLOudr3qQ91cHLUeUKlhiNcxscBpuGr20aZZj6cLQgoF/s640/1.jpg" width="640" /></a></div>
<span tabindex="0"><b>[2,3]=4 toxins</b>: A synthetic strategy that
enables access to four naturally occurring guanidinium toxins, namely
saxitoxin, decarbamoyl saxitoxin, C13‐acetoxy saxitoxin, and
C11‐saxitoxinethanoic acid, is detailed. Highlights of this work include
an unusual Mislow–Evans rearrangement and a late‐stage Stille ketene
acetal cross‐coupling reaction.
</span></div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-6730423182169564762019-01-10T22:17:00.000+05:302019-01-10T22:17:33.987+05:30Ynamide‐Mediated Thiopeptide Synthesis<div dir="ltr" style="text-align: left;" trbidi="on">
Angewchem<br />
<br />
<a href="https://onlinelibrary.wiley.com/doi/10.1002/anie.201811586">Ynamide‐Mediated Thiopeptide Synthesis</a><br />Jinhua Yang, Changliu Wang, Silin Xu, Prof. Dr. Junfeng Zhao<br />
<div class="separator" style="clear: both; text-align: center;">
<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEiB-oxQuIis3gq9mJhyphenhyphen2O2bAieKw40LuOoPkFWrKuR7JlOVoFVwXqCAbiY3t_uPhcphaIVOdTClkitbLYAopkYNjjYl_BcvE2Er9SjWQQWptnrAe55qPIpXL-7yBXIybcq5-rEpYDYbB5p4/s1600/1.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="226" data-original-width="694" height="208" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEiB-oxQuIis3gq9mJhyphenhyphen2O2bAieKw40LuOoPkFWrKuR7JlOVoFVwXqCAbiY3t_uPhcphaIVOdTClkitbLYAopkYNjjYl_BcvE2Er9SjWQQWptnrAe55qPIpXL-7yBXIybcq5-rEpYDYbB5p4/s640/1.jpg" width="640" /></a></div>
<span tabindex="0"><b>Effective to the backbone</b>: In an
ynamide‐mediated two‐step procedure for thiopeptide bond formation,
readily available monothiocarboxylic acids served as thioacyl donors.
The appropriate balance between the activity and stability of
α‐thioacyloxyenamide intermediates formed by the addition of the
monothiocarboxylic acid to the ynamide enabled them to act as effective
thioacylating reagents.
</span></div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-55750722432320856572019-01-10T22:15:00.000+05:302019-01-10T22:15:01.336+05:30Palladium‐Catalyzed Intermolecular [4+1] Spiroannulation by C(sp3)−H Activation and Naphthol Dearomatization <div dir="ltr" style="text-align: left;" trbidi="on">
Angewchem<br />
<br />
<a href="https://onlinelibrary.wiley.com/doi/10.1002/anie.201813202">Palladium‐Catalyzed Intermolecular [4+1] Spiroannulation by C(sp3)−H Activation and Naphthol Dearomatization </a><br />Bojun Tan, Lu Bai, Pin Ding, Jingjing Liu, Yaoyu Wang, Prof. Dr. Xinjun Luan<br />
<div class="separator" style="clear: both; text-align: center;">
<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEjdj3PUHHGkubvoiG9LMI9VmHXv3FWauHy_HkLYsegF6-Oa3umn2fY4kBBIVI4Fb-ABFktkw3Bkruz3N1zGECO3Y_TjSavBTYfYESLfmhZ7Q55urgMAVv6b3v8al6wKdQhJ2LCZqnDexdsL/s1600/1.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="154" data-original-width="726" height="135" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEjdj3PUHHGkubvoiG9LMI9VmHXv3FWauHy_HkLYsegF6-Oa3umn2fY4kBBIVI4Fb-ABFktkw3Bkruz3N1zGECO3Y_TjSavBTYfYESLfmhZ7Q55urgMAVv6b3v8al6wKdQhJ2LCZqnDexdsL/s640/1.jpg" width="640" /></a></div>
<span tabindex="0"><b>Two types of halides</b>: A palladium‐catalyzed
[4+1] spiroannulation of two types of aryl halides has been developed
for the rapid construction of a new class of spirocycles. This
intermolecular domino process was realized through a sequence of C(sp<sup>3</sup>)−H cleavage, unsymmetrical biaryl coupling, and naphthol dearomatization.
</span></div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-7697198748236165252019-01-10T22:12:00.002+05:302019-01-10T22:12:41.689+05:30Carbonylation of Alkyl Radicals Derived from Organosilicates through Visible‐Light Photoredox Catalysis <div dir="ltr" style="text-align: left;" trbidi="on">
Angewchem<br />
<br /><a href="https://onlinelibrary.wiley.com/doi/10.1002/anie.201811858">Carbonylation of Alkyl Radicals Derived from Organosilicates through Visible‐Light Photoredox Catalysis</a><br />
Alex Cartier, Etienne Levernier, Dr. Vincent Corcé, Prof. Takahide Fukuyama, Dr. Anne‐Lise Dhimane, Dr. Cyril Ollivier, Prof. Ilhyong Ryu, Prof. Louis Fensterbank<br />
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<span tabindex="0"><b>Advocating a regime change</b>: Primary,
secondary, and tertiary alkyl radicals, formed by the photocatalyzed
oxidation of organosilicates, underwent three‐component reactions with
carbon monoxide (CO) and radical acceptors to provide unsymmetrical
ketones (see scheme). The concept of radical carbonylation under a
photooxidative regime and metal‐free conditions has significant
potential more generally for photocatalytic carbonylation reactions.</span></div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-91351653157318903942019-01-10T22:09:00.004+05:302019-01-10T22:09:59.777+05:30Oxidative Addition to Palladium(0) Made Easy through Photoexcited‐State Metal Catalysis: Experiment and Computation<div dir="ltr" style="text-align: left;" trbidi="on">
Angewchem<br />
<br />
<a href="https://onlinelibrary.wiley.com/doi/10.1002/anie.201811439">Oxidative Addition to Palladium(0) Made Easy through Photoexcited‐State Metal Catalysis: Experiment and Computation</a><br />Dr. Rajesh Kancherla, Dr. Krishnamoorthy Muralirajan, Dr. Bholanath Maity, Chen Zhu, Patricia E. Krach, Prof. Dr. Luigi Cavallo, Prof. Dr. Magnus Rueping<br />
<div class="separator" style="clear: both; text-align: center;">
<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEi6Pk_NRASBxlclC8flewvSv2OcFqeGFCkivs-e_3kuVPrvmxuAZELGJ3adC2xR_lukzx7qEAGePV6lY_rNVZUWhpIadb4sPApAba7kLLU30QKueO4PkqIQd581e36KdKafcoPaTE6OA4BU/s1600/1.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="232" data-original-width="430" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEi6Pk_NRASBxlclC8flewvSv2OcFqeGFCkivs-e_3kuVPrvmxuAZELGJ3adC2xR_lukzx7qEAGePV6lY_rNVZUWhpIadb4sPApAba7kLLU30QKueO4PkqIQd581e36KdKafcoPaTE6OA4BU/s1600/1.jpg" /></a></div>
<span tabindex="0"><b>Excited‐state palladium</b> catalyzed
decarboxylative alkylation of α,β‐unsaturated acids is achieved by a
barrierless approach under visible light irradiation at room temperature
with good stereoselectivity. Detailed DFT calculations with
experimental evidence suggests a neutral decarboxylative pathway.
</span></div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-10853905878291754092019-01-10T22:06:00.000+05:302019-01-10T22:06:18.330+05:30Late‐Stage Peptide Diversification through Cobalt‐Catalyzed C−H Activation: Sequential Multicatalysis for Stapled Peptides<div dir="ltr" style="text-align: left;" trbidi="on">
Angewchem<br />
<br />
<a href="https://onlinelibrary.wiley.com/doi/10.1002/anie.201811668">Late‐Stage Peptide Diversification through Cobalt‐Catalyzed C−H Activation: Sequential Multicatalysis for Stapled Peptides</a><br />Dr. Mélanie M. Lorion, Nikolaos Kaplaneris, Dr. Jongwoo Son, Dr. Rositha Kuniyil, Prof. Dr. Lutz Ackermann<br />
<div class="separator" style="clear: both; text-align: center;">
<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEjZ8_Y2ilvSU5-4pJvl4b5HIpIHoRiSmOouietFP8U5leVZ-A2YXOiUi2Em8hr-5rSGBBr6F_FZxbKol4Al4I4l1YA0GRJQiilUjrgV0RQLW8sD40ymMfZjw4PICq45ZMSwVx3BRADqnkYg/s1600/1.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="180" data-original-width="890" height="129" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEjZ8_Y2ilvSU5-4pJvl4b5HIpIHoRiSmOouietFP8U5leVZ-A2YXOiUi2Em8hr-5rSGBBr6F_FZxbKol4Al4I4l1YA0GRJQiilUjrgV0RQLW8sD40ymMfZjw4PICq45ZMSwVx3BRADqnkYg/s640/1.jpg" width="640" /></a></div>
<span tabindex="0"><b>C−H activation meets metathesis</b>: Bioorthogonal
C−H activation of peptides was accomplished by using air‐and
moisture‐stable catalysts based on Earth‐abundant cobalt. This reaction
set the stage for the combination of C−H functionalization and olefin
metathesis to construct complex cyclic peptides.
</span></div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-89002245691935943842019-01-10T22:03:00.002+05:302019-01-10T22:03:56.150+05:30Rapid Construction of Structurally Diverse Quinolizidines, Indolizidines, and Their Analogues via Ruthenium‐Catalyzed Asymmetric Cascade Hydrogenation/Reductive Amination<div dir="ltr" style="text-align: left;" trbidi="on">
Angewchem<br /><br /><a href="https://onlinelibrary.wiley.com/doi/10.1002/anie.201812647">Rapid Construction of Structurally Diverse Quinolizidines, Indolizidines, and Their Analogues via Ruthenium‐Catalyzed Asymmetric Cascade Hydrogenation/Reductive Amination</a><br />Ya Chen, Yan‐Mei He, Shanshan Zhang, Tingting Miao, Prof. Dr. Qing‐Hua Fan<br />
<div class="separator" style="clear: both; text-align: center;">
<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhAnNCU2f0GWsHDnrGQavrP3yl7jRm106FGDMevYYPmFVlVN0ViVCtoFsI3i7lFmWqn4ATZvg2wxlVoyhcdA7lHSyNs2-BO4ruj59rU82xPlZaywmlYyrzk5AR2D-P-f5oSCsSQPBXUyZra/s1600/1.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="186" data-original-width="882" height="134" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhAnNCU2f0GWsHDnrGQavrP3yl7jRm106FGDMevYYPmFVlVN0ViVCtoFsI3i7lFmWqn4ATZvg2wxlVoyhcdA7lHSyNs2-BO4ruj59rU82xPlZaywmlYyrzk5AR2D-P-f5oSCsSQPBXUyZra/s640/1.jpg" width="640" /></a></div>
<span tabindex="0"><b>Cascade reaction</b>: A rapid construction of
enantioenriched benzo‐fused quinolizidines, indolizidines, and their
analogues by ruthenium‐catalyzed asymmetric cascade
hydrogenation/reductive amination of quinolinyl‐ and
quinoxalinyl‐containing ketones is described. A range of chiral
benzo‐fused aliphatic <i>N</i>‐heterocyclic compounds were obtained in good yields with excellent enantio‐ and diastereoselectivities (up to >99 % <i>ee</i>, >20:1 dr).
</span></div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-5618386905395500702019-01-10T22:00:00.001+05:302019-01-10T22:00:11.109+05:30A Concise Total Synthesis of (±)‐Vibralactone<div dir="ltr" style="text-align: left;" trbidi="on">
Angewchem<br />
<br />
<a href="https://onlinelibrary.wiley.com/doi/10.1002/anie.201812711">A Concise Total Synthesis of (±)‐Vibralactone</a><br /> Sepand K. Nistanaki, Luke A. Boralsky, Roy D. Pan, Prof. Dr. Hosea M. Nelson<br />
<div class="separator" style="clear: both; text-align: center;">
<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhy4RmCq4pmSaWDzzbnp8Bsz8v_p1RXgkLiQzTQLA9UcaNcTvSQ-SW32_IdY8l8NTkFTWwamm9RBeeqI3N12fJZt-xMtX-3qNHa1ASsuOurufyIf0D9yhZryNetj_XnQ-gpUAzdTzn7ElYQ/s1600/1.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="146" data-original-width="834" height="112" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhy4RmCq4pmSaWDzzbnp8Bsz8v_p1RXgkLiQzTQLA9UcaNcTvSQ-SW32_IdY8l8NTkFTWwamm9RBeeqI3N12fJZt-xMtX-3qNHa1ASsuOurufyIf0D9yhZryNetj_XnQ-gpUAzdTzn7ElYQ/s640/1.jpg" width="640" /></a></div>
<span tabindex="0"><b>Bringing the housane down</b>: The five‐step
synthesis of (±)‐vibralactone, a biologically active terpenoid natural
product, is described. This is the shortest total synthesis of
(±)‐vibralactone reported to date.
</span></div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-20417618111322325522019-01-10T21:57:00.000+05:302019-01-10T21:57:08.804+05:30 The Combination of Benzaldehyde and Nickel‐Catalyzed Photoredox C(sp3)−H Alkylation/Arylation <div dir="ltr" style="text-align: left;" trbidi="on">
Angewchem<br />
<br />
<a href="https://onlinelibrary.wiley.com/doi/10.1002/anie.201810526">The Combination of Benzaldehyde and Nickel‐Catalyzed Photoredox C(sp3)−H Alkylation/Arylation </a><br /> M. Sc. Lumin Zhang, M. Sc. Xiaojia Si, M. Sc. Yangyang Yang, M. Sc. Marc Zimmer, M. Sc. Sina Witzel, Dr. Kohei Sekine, Dr. Matthias Rudolph, Prof. Dr. A. Stephen K. Hashmi<br />
<div class="separator" style="clear: both; text-align: center;">
<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhvaOoesU1M42pU1N1SeHNNvfmcp_6JsNB3Kn2ksvpE6y2RAoJanVWJF9ZC_8xCtQY63LFbGvsdLXRV7lwI32pgg1d8oZomsW6i2jmZcPLWab_yomzogDDVmUs52KcneGP7Y5Lw34kqwNC0/s1600/1.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="142" data-original-width="580" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEhvaOoesU1M42pU1N1SeHNNvfmcp_6JsNB3Kn2ksvpE6y2RAoJanVWJF9ZC_8xCtQY63LFbGvsdLXRV7lwI32pgg1d8oZomsW6i2jmZcPLWab_yomzogDDVmUs52KcneGP7Y5Lw34kqwNC0/s1600/1.jpg" /></a></div>
<span tabindex="0"><b>A combined approach</b>: A simple and general
strategy involving the combination of a photo‐organocatalyst
(benzaldehyde) and a transition‐metal catalyst (nickel) has been
developed for the highly selective photoredox C(sp<sup>3</sup>)−H
alkylation/arylation of ethers. A selective late‐stage modification of
(−)‐ambroxide has also been conducted to demonstrate the applicability
of the method.</span></div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-32741744681051139592019-01-10T21:51:00.002+05:302019-01-10T21:51:59.815+05:30Access to All‐Carbon Spirocycles through a Carbene and Thiourea Cocatalytic Desymmetrization Cascade Reaction<div dir="ltr" style="text-align: left;" trbidi="on">
Angewchem<br />
<a href="https://onlinelibrary.wiley.com/doi/10.1002/anie.201810638"></a><br /><a href="https://onlinelibrary.wiley.com/doi/10.1002/anie.201810638">Access to All‐Carbon Spirocycles through a Carbene and Thiourea Cocatalytic Desymmetrization Cascade Reaction</a><br />Shitian Zhuo, Tingshun Zhu, Liejin Zhou, Chengli Mou, Huifang Chai, Yunpeng Lu, Lutai Pan, Zhichao Jin, Prof. Dr. Yonggui Robin Chi<br />
<br />
<div class="separator" style="clear: both; text-align: center;">
<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEi2Trbc1XSLVHxUcubBT1ZibArB2YWEMxcVPkW3GGaD2QXKZQ1hruyIkvUQRSiyyhm2UuCqNzMliYmMlDotrY3nSKR_i-4YHJ-0vRppycsgHg7bFjVTdt-jc5qSqtNRZMX1nsmEbhlENbN8/s1600/1.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="216" data-original-width="752" height="183" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEi2Trbc1XSLVHxUcubBT1ZibArB2YWEMxcVPkW3GGaD2QXKZQ1hruyIkvUQRSiyyhm2UuCqNzMliYmMlDotrY3nSKR_i-4YHJ-0vRppycsgHg7bFjVTdt-jc5qSqtNRZMX1nsmEbhlENbN8/s640/1.jpg" width="640" /></a></div>
<span tabindex="0"><b>Harmony between cats</b>: Dual carbene and
thiourea catalysis enabled rapid asymmetric access to spirocyclic
compounds by a desymmetrization process (see scheme). The presence of
the thiourea cocatalyst was essential for this carbene‐catalyzed
enantioselective synthesis of all‐carbon spirocycles to proceed. The
reaction products can be readily transformed into sophisticated
multicyclic molecules and chiral ligands.</span></div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-44635887019019684002019-01-10T21:48:00.000+05:302019-01-10T21:48:17.020+05:30 Chiral Sulfide Catalysis for Desymmetrizing Enantioselective Chlorination<div dir="ltr" style="text-align: left;" trbidi="on">
Angewchem<br />
<br /><a href="https://onlinelibrary.wiley.com/doi/10.1002/anie.201811621">Chiral Sulfide Catalysis for Desymmetrizing Enantioselective Chlorination</a><br /> Qingxiang Cao, Jie Luo, Prof. Dr. Xiaodan Zhao<br />
<br />
<div class="separator" style="clear: both; text-align: center;">
<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEjkI0xamuMpyVOdUtG6BrGz6FvE-aF6dhtLqgBI0PzNSC4cxNpeGpaA6JIyirpElXc20VcrGK3YFCb9S55ZgbGnAvfZ89GodyQ2ucThlyaUL9QueD6S9aGhHpEMiaDIEnLx-TTKgZjw79Q3/s1600/1.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="202" data-original-width="552" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEjkI0xamuMpyVOdUtG6BrGz6FvE-aF6dhtLqgBI0PzNSC4cxNpeGpaA6JIyirpElXc20VcrGK3YFCb9S55ZgbGnAvfZ89GodyQ2ucThlyaUL9QueD6S9aGhHpEMiaDIEnLx-TTKgZjw79Q3/s1600/1.jpg" /></a></div>
<span tabindex="0"><b>A chiral sulfide</b> catalyzed the desymmetrizing
enantioselective chlorination of various aryl‐tethered diolefins and
diaryl‐tethered olefins to afford teralins and tricyclic
hexahydrophenalene derivatives, respectively, bearing multiple
stereogenic centers. In contrast, the tertiary amine catalyst (DHQD)<sub>2</sub>PHAL led to a diastereomeric product. The products could be transformed into diverse compounds such as spiro‐N‐heterocycles.
</span></div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-40344669631993093632019-01-10T21:45:00.000+05:302019-01-10T21:45:12.412+05:30 Catalyst‐Controlled 1,2‐ and 1,1‐Arylboration of α‐Alkyl Alkenyl Arenes <div dir="ltr" style="text-align: left;" trbidi="on">
Angewchem<br />
<a href="https://onlinelibrary.wiley.com/doi/abs/10.1002/anie.201812533" target="_blank"><br /></a>
<a href="https://onlinelibrary.wiley.com/doi/abs/10.1002/anie.201812533" target="_blank">Catalyst‐Controlled 1,2‐ and 1,1‐Arylboration of α‐Alkyl Alkenyl Arenes </a><br />Allison M. Bergmann, Stanna K. Dorn, Kevin B. Smith, Kaitlyn M. Logan Prof. M. Kevin Brown<br />
<br />
<div class="separator" style="clear: both; text-align: center;">
<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEi-ESI2lF2jyjXUP31TkRwfWli3IhMHvLtWMfnJv27HglAfCVD0gNAWCAYjv1Lse4AgUPIpJtNqWc1YZSTnP65PVGvM92MvSnHtpIzFfIqaWmV3KNcvxL5QOjv7-yMBChSujpH9h8CFgYK2/s1600/1.jpg" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="216" data-original-width="630" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEi-ESI2lF2jyjXUP31TkRwfWli3IhMHvLtWMfnJv27HglAfCVD0gNAWCAYjv1Lse4AgUPIpJtNqWc1YZSTnP65PVGvM92MvSnHtpIzFfIqaWmV3KNcvxL5QOjv7-yMBChSujpH9h8CFgYK2/s1600/1.jpg" /></a></div>
Two methods are reported for the 1,2‐ and 1,1‐arylboration of α‐methyl
vinyl arenes. In the case of 1,2‐arylboration, the formation of a
quaternary center occurred through a rare cross‐coupling reaction of a
tertiary organometallic complex. 1,1‐Arylboration was enabled by
catalyst optimization and occurred through a β‐hydride
elimination/reinsertion cascade. Enantioselective variants of both
processes are presented as well as mechanistic investigations.<br />
</div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-17143449826562060302018-10-26T11:58:00.000+05:302018-10-26T11:58:00.308+05:30Palladium‐Catalyzed Divergent Cyclopropanation by Regioselective Solvent‐Driven C(sp3)−H Bond Activation<div dir="ltr" style="text-align: left;" trbidi="on">
Angewchem<br />
<br />
<a href="https://onlinelibrary.wiley.com/doi/abs/10.1002/anie.201809133" target="_blank">Palladium‐Catalyzed Divergent Cyclopropanation by Regioselective Solvent‐Driven C(sp3)−H Bond Activation</a><br /><br />Da Sol Chung, Jae Sung Lee, Ho Ryu, Dr. Jiyong Park, Hyunjoong Kim, Joo Hyun Lee, Dr. U Bin Kim, Prof. Dr. Won Koo Lee, Prof. Dr. Mu‐Hyun Baik, Prof. Dr. Sang‐gi Lee<div>
<br /></div>
<div class="separator" style="clear: both; text-align: center;">
<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEitz7k3UwplYf4url-2nMi4bDGJ5swstCo3C3Wr9_6aw40FPV-i-SdS5_871ZKoTDSr4FYQKPHqP79lje65KQLjJY2fifrvCyfOwPIG_h7qx6xccUUp3l80EqsH7n7o3zDL8Z-I0xur8xIp/s1600/1.webp" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><img border="0" data-original-height="262" data-original-width="432" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEitz7k3UwplYf4url-2nMi4bDGJ5swstCo3C3Wr9_6aw40FPV-i-SdS5_871ZKoTDSr4FYQKPHqP79lje65KQLjJY2fifrvCyfOwPIG_h7qx6xccUUp3l80EqsH7n7o3zDL8Z-I0xur8xIp/s1600/1.webp" /></a></div>
<div>
<br /></div>
<div style="text-align: justify;">
<span style="background-color: white; color: #1c1d1e; font-family: "Open Sans", sans-serif, icomoon; font-size: 16px;">A tandem palladium‐catalyzed Heck/regioselective C(sp</span><span style="background-color: white; box-sizing: border-box; color: #1c1d1e; font-family: "Open Sans", sans-serif, icomoon; font-size: 12px; line-height: 0; position: relative; top: -0.5em; vertical-align: baseline;">3</span><span style="background-color: white; color: #1c1d1e; font-family: "Open Sans", sans-serif, icomoon; font-size: 16px;">)−H activation reaction for the divergent synthesis of spiro‐ and fused‐cyclopropanated indolines from </span><i style="background-color: white; box-sizing: border-box; color: #1c1d1e; font-family: "Open Sans", sans-serif, icomoon; font-size: 16px;">N</i><span style="background-color: white; color: #1c1d1e; font-family: "Open Sans", sans-serif, icomoon; font-size: 16px;">‐methallylated 2‐bromoarylamides. The regioselectivity of the C−H bond activation in the σ‐alkylPd</span><span style="background-color: white; box-sizing: border-box; color: #1c1d1e; font-family: "Open Sans", sans-serif, icomoon; font-size: 12px; line-height: 0; position: relative; top: -0.5em; vertical-align: baseline;">II</span><span style="background-color: white; color: #1c1d1e; font-family: "Open Sans", sans-serif, icomoon; font-size: 16px;"> intermediate is controlled by the solvent used.</span></div>
</div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-15331676187812391152018-10-26T11:54:00.005+05:302018-10-26T11:54:34.754+05:30Total Synthesis of an Atropisomer of the Schisandra Triterpenoid Schiglautone A<div dir="ltr" style="text-align: left;" trbidi="on">
Angewchem<br />
<br /><a href="https://onlinelibrary.wiley.com/doi/abs/10.1002/anie.201809076" target="_blank">Total Synthesis of an Atropisomer of the Schisandra Triterpenoid Schiglautone A</a><br /><br />Binjie Ma, Yifan Zhao, Dr. Chi He, Prof. Dr. Hanfeng Ding<div class="separator" style="clear: both; text-align: center;">
<a href="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEgVTq0ExzNeMKnkDQXlP8gs8LsGMtfONtIGO-mrUkJE_RwICsEFm5nIVnO47xkVpz_STlhwy-97d5vEb9Xr5P39qHjiEeWMCTuud5dGWzA8Gk0yUPYLzVhEUre44lb8Z_ZHwtaAxxu5gR5J/s1600/1.webp" imageanchor="1" style="margin-left: 1em; margin-right: 1em;"><br /><img border="0" data-original-height="186" data-original-width="670" src="https://blogger.googleusercontent.com/img/b/R29vZ2xl/AVvXsEgVTq0ExzNeMKnkDQXlP8gs8LsGMtfONtIGO-mrUkJE_RwICsEFm5nIVnO47xkVpz_STlhwy-97d5vEb9Xr5P39qHjiEeWMCTuud5dGWzA8Gk0yUPYLzVhEUre44lb8Z_ZHwtaAxxu5gR5J/s1600/1.webp" /></a></div>
<div>
<br /><div>
<span style="background-color: white; color: #1c1d1e; font-family: "Open Sans", sans-serif, icomoon; font-size: 16px; text-align: justify;">A diastereoselective approach for the total synthesis of an unusual atropisomer of the Schisandra triterpenoid (±)‐schiglautone A is described. The efficient synthetic strategy features three key transformations: 1) two sequential titanium(III)‐catalyzed radical cyclization/homologation reactions to construct the </span><i style="background-color: white; box-sizing: border-box; color: #1c1d1e; font-family: "Open Sans", sans-serif, icomoon; font-size: 16px; text-align: justify;">trans</i><span style="background-color: white; color: #1c1d1e; font-family: "Open Sans", sans-serif, icomoon; font-size: 16px; text-align: justify;">‐fused [6,7] bicycle as well as install the quaternary carbons at C10 and C14 with the desired stereochemistry; 2) a Claisen rearrangement followed by a ring‐closing metathesis to forge the strained nine‐membered ring; and 3) a substrate‐controlled Michael addition to enable the introduction of the C17 side‐chain with good diastereoselectivity.</span></div>
</div>
</div>
Unknownnoreply@blogger.com0tag:blogger.com,1999:blog-1866422029659903041.post-48593342256395525232018-10-26T11:49:00.002+05:302018-10-26T11:49:27.294+05:30Synthesis of Functionalized Cyclopropanes from Carboxylic Acids by a Radical Addition–Polar Cyclization Cascade<div dir="ltr" style="text-align: left;" trbidi="on">
Angewchem<br />
<br /><a href="https://onlinelibrary.wiley.com/doi/abs/10.1002/anie.201808598" target="_blank">Synthesis of Functionalized Cyclopropanes from Carboxylic Acids by a Radical Addition–Polar Cyclization Cascade</a><br /><br />Dr. Chao Shu, Riccardo S. Mega Björn, J. Andreassen, Dr. Adam Noble, Prof. Dr. Varinder K. Aggarwal<div>
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<span style="background-color: white; color: #1c1d1e; font-family: "Open Sans", sans-serif, icomoon; font-size: 16px;">The development of a photoredox‐catalyzed decarboxylative radical addition–polar cyclization cascade approach to functionalized cyclopropanes. Reductive termination of radical–polar crossover reactions between aliphatic carboxylic acids and electron‐deficient alkenes yielded carbanion intermediates that were intercepted in intramolecular alkylations with alkyl chlorides appended to the alkene substrate.</span></div>
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