Copper(ii) catalyzed domino synthesis of quinoline derivatives from arylamines and alkynes

Abstract

The Cu(OAc)₂·H₂O catalyzed domino reaction of primary arylamines and electron-deficient terminal alkynes was developed at room temperature. It provides a convenient access to a variety of 2,4-disubstituted quinolines in good to excellent yields without protection from moisture or air. Control experiments suggest that the reaction might be initiated from alkyne homocoupling, followed by copper catalyzed hydroamination and cyclization.