I₂/TBHP-Catalyzed Chemoselective Amination of Indoles

Abstract

A novel I2/TBHP-mediated direct oxidative diamination reaction of indoles with anilines was developed. The reaction proceeded smoothly under aqueous and open air reaction conditions. This protocol provides a practical synthetic method for the synthesis of Tryptanthrin and the construction of N-C3 linked pyrrolidinoindolines which is the core structure of Psychotrimine.