Copper-catalyzed Tandem Cyclization to Access 4-Aminoquinoline Derivatives

An efficient and practical method for the synthesis of 4-aminoquinoline derivatives has been developed via copper-catalyzed cascade cyclization of 2-aminobenzonitrile and nitroolefins. This reaction proceeds through a consecutive Michael addition/cyclization/oxidization protocol, providing 4-aminoquinolines with moderate to excellent yields under mild conditions. This method features readily available materials, one-pot one-step operation, and proceeds without bases.