A Facile Synthesis of Quinazolin-4(3H)-ones via Copper-Catalyzed One-Pot, Three-Component Tandem Reaction

Abstract

A simple and convenient one-pot, three-component tandem reaction has been developed for the synthesis of substituted quinazolin-4(3H)-ones using CuI/L-proline as catalytic system. A series of 35 quinazolin-4(3H)-ones was synthesized in good to high yield. The method involves copper-catalyzed double C−N coupling, reductive amination, condensation, cyclization and aerobic oxidation. Good functional group tolerance, mild reaction condition, readily available starting materials and user friendly procedure makes this protocol practically good and attractive method for the synthesis of quinazolin-4(3H)-ones.