Copper-Catalyzed Sequential Ullmann N-Arylation and Aerobic Oxidative C–H Amination: A Convenient Route to Indolo[1,2-c]quinazoline Derivatives

An efficient synthesis of indolo[1,2-c]quinazoline derivatives has been developed by copper-catalyzed sequential Ullmann N-arylation and aerobic oxidative C-H amination. The protocol uses readily available 2-(2-halophenyl)-1H-indoles and (aryl)methanamines as the starting materials to afford indolo[1,2-c]quinazolines, which are the core units of hinckdentine A.