Copper-catalyzed N-arylation and aerobic oxidation: one-pot synthesis of tetrahydroisoquinolino[2,1-a]quinazolinone derivatives

An efficient and practical copper-catalyzed one-pot method for synthesis of tetrahydroisoquinolino[2,1-a]quinazolinone derivatives has been developed, and the corresponding target products were prepared in moderate to good yields. The one-pot approach underwent sequential copper-catalyzed N-arylation, intramolecular aerobic oxidative cyclization, and the newly synthesized products provided diverse structures for screening of biological molecules.