Rh(iii)-catalyzed synthesis of 1-aminoindole derivatives from 2-acetyl-1-arylhydrazines and diazo compounds in water

Abstract

A novel and direct approach to synthesize 1-aminoindole derivatives by Rh(III)-catalyzed cyclization of 2-acetyl-1-arylhydrazines with diazo compounds via aryl C–H activation has been developed. This intermolecular annulation involving tandem C–H activation, cyclization and condensation steps proceeds efficiently in water, obviates the need of external oxidants, and displays a broad substituent scope.