Efficient copper-catalyzed amination of aryl halides with amines and NH heterocycles using rac-BINOL as ligand

A highly efficient copper-catalyzed system using commercially available racemic 1,1′-binaphthyl-2,2′-diol (rac-BINOL) as the ligand was developed for amination of aryl halides and heteroaryl halides with alkyl amines and NH heterocycles. Good to high yields were obtained for aryl bromides and heteroaryl chlorides. The commercially available rac-BINOL ligand with excellent stability and high efficiency for aryl bromides and heteroaryl chlorides ultimately make this protocol of potentially practical utility.