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| Research progress on Difluoromethyl-containing drugs and Difluoromethylation reagents |
| TAO Xuefen ZHANG Ying ZHENG Jiefeng WANG Yuxin JIN Yinxiu TANG Fuqin |
| School of Medicine and Pharmaceutical Engineering, Taizhou Vocational ＆ Technical College, Zhejiang Province, Taizhou 310008, China |
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Abstract This paper presentes all Difluoromethyl-containing drugs approved by FDA in the United States from 2011 to 2018 for the first time. And briefly introduces their clinical applications. The Difluoromethylation reagents reported domestic and foreign are reviewed and classified based on their electrical effect. Among them, the nucleophilic difluoromethylation reagents are the most common ones. They mainly include TMS, PhXCF2H, BrCF2PO(OEt)2, Phenylsulfonyl and Phenylsulfonyl Difluoroacetic acid metal salts. The researches on electrophilic Difluoromethylation reagents are relatively fewer. Difluoromethyl radical donors and Difluorometallic salts have been reported.
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