Copper-catalyzed intermolecular amidation of 8-methylquinolines with N-fluoroarylsulfonimides via Csp3-H activation

作者：Zhang, Xiaolei; Wu, Rui; Liu, Wanyi; Qian, Dang-Wei; Yang, Jinhui; Jiang, Pengju; Zheng, Qing-Zhong^*

来源：Organic and Biomolecular Chemistry, 2016, 14(21): 4789-4793.

DOI：10.1039/c6ob00553e

• C-H AMINATION
• UNACTIVATED C(SP(3))-H BONDS
• INTRAMOLECULAR C(SP(3))-H
• STEREOSELECTIVE-SYNTHESIS
• HETEROCYCLE SYNTHESIS
• FUNCTIONAL MOLECULES
• AMINO-ACIDS
• FLUOROBENZENESULFONIMIDE
• ALKYLATION
• ACRIDINES

An efficient copper-catalyzed C-H amidation of 8-methylquinolines with N-fluoroarylsulfonimides via Csp(3)-H activation is described. The reaction proceeds with high functional group tolerance, providing a novel approach to valuable quinolin-8-ylmethanamine derivatives in the absence of an additional oxidant.

• 单位
  天然药物与仿生药物国家重点实验室; 宁夏大学; 北京大学