Facile one-pot synthesis of 2-aminoindoles from simple anilines and ynamides

Abstract

A highly effective and straightforward one-pot synthesis of diversely substituted 2-aminoindoles has been developed, involving sequential Au(I)-catalyzed regioselective hydroamination and CuCl2-mediated oxidative cyclization. This protocol offers an operationally easy, simple, robust, and sustainable approach with the use of readily available starting materials, good functional group tolerance, and high practicality and efficiency.