Cu-catalyzed N-alkylation of aliphatic amines with enantioconvergence.
Researchers have developed a new method for the enantioselective N-alkylation of aliphatic amines with α-carbonyl alkyl chlorides using chiral tridentate anionic ligands and copper catalysts. The method can convert feedstock chemicals, including ammonia and pharmaceutically-relevant amines, into unnatural chiral α-amino amides under mild and robust conditions with excellent enantioselectivity and functional group tolerance. The method has potential applications in the expedited synthesis of diverse amine drug molecules.