Enantioselective amine α-functionalization via palladium-catalysed C–H arylation of thioamides

Enantioselective amine α-functionalization via palladium-catalysed C–H arylation of thioamides
Pankaj Jain, Pritha Verma, Guoqin Xia & Jin-Quan Yu
Nature Chemistry doi:10.1038/nchem.2619
Chiral, saturated N-heterocycles are prized as pharmaceutical agents and chiral auxiliaries, but are challenging to access without using prefunctionalized starting materials. Now, chiral phosphoric acids are found to enable the enantioselective Pd(II)-catalysed arylation of α-methylene C–H bonds in a wide variety of amines using thioamide as the directing group.

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