Cu-Catalyzed Intermolecular γ-Site C-H Amination of Cyclohexenone Derivatives: The Benefit of Bifunctional Ligands

Utilizing 1,10-phenanthroline-type bifunctional ligands, an efficient Cu-catalyzed intermolecular site-selective remote C-H amination using cyclohexenone derivatives and anilines was realized. The amide group installed on the bifunctional ligand played a key role in stabilizing the N-centered radical generated in situ to realize C-N-directed formation. Meanwhile, a useful catalytic system for site-selective intermolecular remote gamma-C-H amination to p-aminophenols and gamma-aminated enones was established. This economical and practical approach using oxygen as the terminal oxidant was mild and environmentally friendly.