Copper-catalyzed enantioselective intramolecular N-arylation, an efficient method for kinetic resolutions.

For the first time, copper-catalyzed intramolecular N-arylation was successfully applied to the kinetic resolution strategy. Under the catalysis of CuI-BINOL derived ligands, the kinetic resolution of rac-2-amino-3-(2-iodoaryl)propionates and rac-2-amino-4-(2-iodoaryl)butanoates afforded chiral intramolecular coupling products and recovered the starting materials in high enantioselectivity (s factors up to 245).