Journal
CHINESE JOURNAL OF ORGANIC CHEMISTRY
Volume 38, Issue 7, Pages 1569-1585Publisher
SCIENCE PRESS
DOI: 10.6023/cjoc201801041
Keywords
drifluoromethyl; nucleophilic reagent; electrophilic reagent; difluorocarbene; direct difluoromethylation
Categories
Funding
- Key Research and Development Projects of Shanxi Province [2017ZDXM-GY-042, 2017ZDXM-GY-070]
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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.
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