Design and application of a novel and effective ligand for the Cu-catalyzed amination of aryl halides in water

An effective ligand for the Ullmann-type C-N coupling reaction in water has been obtained using a novel tactic, namely, introducing a third group into the ligand to both improve the ligand's water solubility and enhance the ligand's coordinating ability. Applying this method, we have developed an effective ligand for the Cu-catalyzed amination of aryl halides, in particular, for aryl chlorides in water. The substrate diversity of the catalyst system, relatively less time required (6-12 h), and water as the reaction solvent make it attractive in both academia and industry.