Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (7): 1569-1585.DOI: 10.6023/cjoc201801041 Previous Articles     Next Articles

Reviews

二氟甲基化方法研究进展

王为强, 余秦伟, 张前, 李江伟, 惠丰, 杨建明, 吕剑   

  1. 西安近代化学研究所 氟氮化工资源高效开发与利用国家重点实验室 西安 710065
  • 收稿日期:2018-01-28 修回日期:2018-04-02 出版日期:2018-07-25 发布日期:2018-04-27
  • 通讯作者: 杨建明, 吕剑 E-mail:yangjm204@163.com;lujian204@263.net
  • 基金资助:

    陕西省重点研发计划(Nos.2017ZDXM-GY-042,2017ZDXM-GY-070)资助项目.

Recent Progress on Difluoromethylation Methods

Wang Weiqiang, Yu Qinwei, Zhang Qian, Li Jiangwei, Hui Feng, Yang Jianming, Lü Jian   

  1. State Key Laboratory of Fluorine & Nitrogen Chemicals, Xi'an Modern Chemistry Research Institute, Xi'an 710065
  • Received:2018-01-28 Revised:2018-04-02 Online:2018-07-25 Published:2018-04-27
  • Contact: 10.6023/cjoc201801041 E-mail:yangjm204@163.com;lujian204@263.net
  • Supported by:

    Project supported by the Key Research and Development Projects of Shanxi Province (Nos. 2017ZDXM-GY-042, 2017ZDXM-GY-070).

The difluoromethyl functional group (CF2H) which has strong lipophilic and electron-withdrawing properties can significantly enhance the physiological activity of organic molecules. The applications of CF2H-containing compounds in the fields of drugs, agrochemicals and so on have attracted great attention of many research groups. Therefore, the development of effective and general methodologies for the selective incorporation of difluoromethyl groups has become one of the hotspots in the field of organic chemistry. Recently, new difluoromethylation reagents and methods that were able to efficiently incorporate the difluoromethyl group under mild conditions have been developed rapidly, that pave the way for the facile introduction of difluoromethyl group into site-specific positions of the target molecules. In this paper, we will first briefly introduce some organic molecules with different functional groups which can be difluoromethylated, and then focus on the development of the recent high-performance difluoromethylation reagents, new reactions and catalysts. Finally, we will discuss the remaining problems and challenges in this particular field.

Key words: drifluoromethyl, nucleophilic reagent, electrophilic reagent, difluorocarbene, direct difluoromethylation