Rhodium-Catalyzed Regioselective C–H Chlorination of 7-Azaindoles Using 1,2-Dichloroethane

Abstract

An unexpected rhodium-catalyzed regioselective C-H chlorination of 7-azaindoles was developed using 1,2-dichloroethane (DCE) as a chlorinating agent and 7-azaindole as the directing group. This protocol provides an efficient access to ortho-chlorinated azaindoles with operational simplicity, good functional group tolerance, and a wide substrate scope.