Copper-Catalyzed Aerobic Intramolecular Carbo- and Amino-Oxygenation of Alkynes for Synthesis of Azaheterocycles

A synthetic method of highly substituted quinolines has been developed from N-(2-alkynylaryl)enamine carboxylates under Cu-catalyzed aerobic conditions via intramolecular carbo-oxygenation of alkynes. This strategy was further applied for N-alkynylamidines for amino-oxygenation of alkynes, leading to imidazole and quinazoline derivatives.