Synthesis of Azepinoindoles via Pd-Catalyzed C(sp2)–H Imidoylative Cyclization Reactions

An efficient and convenient method for the construction of diverse free (N-H)-benzazepinoindoles by Pd-catalyzed C(sp2)-H imidoylative cyclization of 3-(2-isocyanobenzyl)-1H-indoles was developed. The reaction shows a wide substrate scope and can be scaled up, providing a practical route to valuable bioactive azepinoindoles.