Organocatalytic and Highly Enantioselective Direct α-Amination of Aromatic Ketones

Abstract

The first highly enantioselective direct alpha-amination of aryl ketones was reported to be catalyzed by organic primary amines derived from cinchona alkaloids. Excellent enantioselectivities (88-99% ee) have been achieved for a broad spectrum of aryl ketones. The presence of 4 A molecular sieves was of great assistance for the high conversions and enantiocontrol.