Iron–iodine co-catalysis towards tandem C–N/C–C bond formation: one-pot regioselective synthesis of 2-amino-3-alkylindoles

Abstract

Herein, we report a novel iron and iodine cooperative catalytic system for intermolecular C2,3-H aminoalkylation of indoles with azoles and xanthenes as the coupling agents, which allows tandem C–N/C–C bond formation, two steps in one pot, towards the regioselective synthesis of diverse 2-amino-3-alkylindoles with the features of good substrate and functional group compatibility, and readily available catalyst system and feedstocks. The new protocol offers great potential for the discovery of further biological activities.