Copper-Catalyzed Selective ortho-C–H/N–H Annulation of Benzamides with Arynes: Synthesis of Phenanthridinone Alkaloids

An efficient and convenient copper-catalyzed method has been developed to achieve direct ortho-C–H/N-H annulation to synthesize phenanthridinones with arynes. This method highlights an emerging strategy to transform inert C–H bonds into versatile functional groups in organic synthesis and provides a new way to synthesize phenanthridinone alkaloids efficiently.