Copper-catalyzed synthesis of quinazoline derivatives via Ullmann-type coupling and aerobic oxidation.

A simple and efficient copper-catalyzed approach to quinazoline derivatives has been developed, and the protocol uses readily available substituted (2-bromophenyl)methylamines and amides as the starting materials, and the cascade reactions were performed under air via sequential Ullmann-type coupling and aerobic oxidation without addition of any ligand or additive. The present method provides a convenient and practical strategy for synthesis of quinazoline derivatives.