A new strategy for direct and highly efficient synthesis of 2,3'-bisindolin-3-ones has been developed via a gold/copper-co-catalyzed tandem reactions of 2-alkynylanilines using TBHP as the terminal oxidant and oxygen-atom source. The single-step process involves a novel tandem intermolecular nucleophilic addition, intramolecular cyclization/oxidative cross-dehydrogenative coupling where up to four new bonds and two indole rings were created simultaneously in one-pot manner. The reaction features a broad substrate scope, good functional group tolerance, and high atom-economy.

A novel acid/base-co-catalyzed direct intermolecular a-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 aamino enones and benzodiazepine derivatives in a single step.