Cu-Catalyzed Synthesis of C-3 Dicarbonyl Indoles via Aerobic Oxidative Coupling of Acetophenones with Indoles

A Cu-catalyzed aerobic oxidative coupling of acetophenones with indoles has been developed, and is an efficient and practical C-H (sp(3)) functionalization approach to C-3 dicarbonyl indoles, using O-2 as the green oxidant. Moreover, a series of dicarbonyl indoles have been obtained smoothly and the plausible mechanism is proposed based on control experiments.