Citation: Wang Weiqiang, Yu Qinwei, Zhang Qian, Li Jiangwei, Hui Feng, Yang Jianming, Lü Jian. Recent Progress on Difluoromethylation Methods[J]. Chinese Journal of Organic Chemistry, ;2018, 38(7): 1569-1585. doi: 10.6023/cjoc201801041 shu

Recent Progress on Difluoromethylation Methods

State Key Laboratory of Fluorine & Nitrogen Chemicals, Xi'an Modern Chemistry Research Institute, Xi'an 710065

Corresponding author: Yang Jianming, yangjm204@163.com Lü Jian, lujian204@263.net
Received Date: 28 January 2018
Revised Date: 2 April 2018
Available Online: 27 July 2018
Fund Project: Project supported by the Key Research and Development Projects of Shanxi Province (Nos. 2017ZDXM-GY-042, 2017ZDXM-GY-070)the Key Research and Development Projects of Shanxi Province 2017ZDXM-GY-042the Key Research and Development Projects of Shanxi Province 2017ZDXM-GY-070

Figures(29)

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.
- drifluoromethyl,
- nucleophilic reagent,
- electrophilic reagent,
- difluorocarbene,
- direct difluoromethylation
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