Copper-Catalyzed Ligand-Free Remote C-H Bond Amidation of 8-Amidoquinolines with N-Fluorobenzenesulfonimide

A copper-catalyzed direct C-H bond C5-amidation of 8-amidoquinolines with NFSI has been developed. This catalytic amination process is carried out without any ligands to form various derivatives in moderate to excellent yields using a commercially available Cu(II) as the catalyst under a simple condition. A single-electron transfer (SET)-mediated mechanism was proposed based on the experimental data and a serious of mechanistic studies.

Automated summary

A copper-catalyzed direct C-H bond C5-amidation of 8-amidoquinolines with NFSI has been developed, which does not require any ligands and can form various derivatives in moderate to excellent yields using a commercially available Cu(II) catalyst under simple conditions. A single-electron transfer (SET)-mediated mechanism was proposed based on experimental data and a series of mechanistic studies.