摘要

A novel acid/base-co-catalyzed direct intermolecular alpha-amination of various cyclic ketones has been developed for the first time. The reaction employs molecular oxygen as the sole oxidant under metal-free conditions. The reaction tolerates a wide range of various anilines, especially primary diamine derivatives, and provides a simple and efficient method for the constructions of alpha-amino enones and benzodiazepine derivatives in a single step.