Abstract The Buchwald–Hartwig coupling/Michael addition sequence has been successfully applied to the synthesis of functionalized 1, 2-disubstituted 4-quinolones using Pd (OAc) 2 as a catalyst and PPh 3 as a ligand. Under these conditions, the intermediate products first formed from chalcones and primary amines underwent catalytic dehydrogenation to yield the 1, 2-disubstituted 4-quinolones.