Copper-Catalyzed Regioselective sp3 C–H Azidation of Alkyl Substituents of Indoles and Tetrahydrocarbazoles

An efficient regioselective sp3 C–H azidation is developed using CuBr as the catalyst and Zhdankin azidoiodinane as the “N3” source. Under simple and mild reaction conditions, the azido group could be successfully incorporated into the sp3 C–H alkyl substituents of indoles and tetrahydrocarbazoles.