Chin. J. Org. Chem. ›› 2017, Vol. 37 ›› Issue (12): 3060-3075.DOI: 10.6023/cjoc201709011 Previous Articles     Next Articles

Reviews

三氟甲基亚磺酸钠实现的三氟甲基化反应研究进展

惠人杰, 张士伟, 谭政, 吴小培, 冯柏年   

  1. 江南大学药学院 无锡 214122
  • 收稿日期:2017-09-08 修回日期:2017-11-09 发布日期:2017-12-08
  • 通讯作者: 冯柏年 E-mail:fengbainian@jiangnan.edu.cn
  • 基金资助:

    江苏省自然科学基金(No.BK20140136)及江苏高校品牌专业建设工程(No.PPZY2015B146)资助项目.

Research Progress of Trifluoromethylation with Sodium Trifluoromethanesulfinate

Hui Renjie, Zhang Shiwei, Tan Zheng, Wu Xiaopei, Feng Bainian   

  1. School of Pharmaceutical Science, Jiangnan University, Wuxi 214122
  • Received:2017-09-08 Revised:2017-11-09 Published:2017-12-08
  • Contact: 10.6023/cjoc201709011 E-mail:fengbainian@jiangnan.edu.cn
  • Supported by:

    Project supported by the Natural Science Foundation of Jiangsu Province (No. BK20140136) and the Top-notch Academic Programs Project of Jiangsu Higher Education Institutions (No. PPZY2015B146).

Trifluoromethyl can increase the chemical and metabolic stability of drugs, improve its lipophilicity and bioavailability, and furthermore, enhance drug binding selectivities. Sodium trifluoromethanesulfinate (CF3SO2Na) is a stable inexpensive reagent, which has been widely used in the field of organic fluorine chemistry. The recent progress (2014~2017) in trifluoromethylation by employing CF3SO2Na as the trifluoromethyl source is summarized. In addition, the reactions of bifunctionalization, trifluoromethylation of aromatics, trifluoromethylthioization and other types of reactions are described respectively, with their applications and reaction mechanism. It is hoped that this review can be referred to in the studies of trifluoromethyl introduction.

Key words: sodium trifluoromethanesulfinate, trifluoromethylation, mechanism