Chinese Journal of Organic Chemistry ›› 2020, Vol. 40 ›› Issue (3): 724-730.DOI: 10.6023/cjoc201908036 Previous Articles     Next Articles


郭圆圆a, 刘振伟a, 朱明祥a, 李琳琳a, 李敬亚b, 邹大鹏a, 吴豫生b, 吴养洁a   

  1. a 郑州大学化学与分子工程学院 郑州 450052;
    b 郑州泰基鸿诺医药股份有限公司 郑州 450052
  • 收稿日期:2019-08-27 修回日期:2019-11-05 发布日期:2020-04-02
  • 通讯作者: 邹大鹏, 吴豫生, 吴养洁;;
  • 基金资助:

Copper-Promoted Dimethylthiolation of Benzamides under Assistance of 8-Aminoquinoline Group

Guo Yuanyuana, Liu Zhenweia, Zhu Mingxianga, Li Linlina, Li Jingyab, Zou Dapenga, Wu Yushengb, Wu Yangjiea   

  1. a College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou 450052;
    b Tetranov Biopharm, LLC, Zhengzhou 450052
  • Received:2019-08-27 Revised:2019-11-05 Published:2020-04-02
  • Supported by:
    Project supported by the National Natural Science Foundation of China (Nos. 21172200, 21702191).

Cu(II)-promoted dimethylthiolation of C(sp2)-H bonds using DMSO as the methylthiolation source with the assistance of an 8-aminoquinoline directing group have been developed. A number of dimethylthiolated benzamides were efficiently synthesized using CuSO4·5H2O as a promoter in moderate to good yields. In addition, this reaction system features facile conditions and no other oxidant additive was required.

Key words: Dimethylthiolation, DMSO, 8-Aminoquinoline, Copper-promoted