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N-Difluoromethylation of imidazoles and pyrazoles using BrCF2PO(OEt)2 under mild condition
Authors:Ting Mao  Liang Zhao  Yang Huang  Yue-Guang Lou  Qiuli Yao  Xiao-Fei Li  Chun-Yang He
Affiliation:Generic Drug Research Center of Guizhou Province, School of Pharmacy, Zunyi Medical University, No 6 West Xuefu Road, Zunyi, Guizhou 563003, China
Abstract:A simple and efficient protocol for the direct N-difluoromethylation of imidazoles and pyrazoles has been developed. The reaction makes use of commercially available, non-ozone-depleting and easy handling BrCF2PO(OEt)2 as difluorocarbene precursor, and provides a cost-efficient and environmentally benign access to some difluoromethylated biologically relevant molecules.
Keywords:Difluoromethylation  Difluorocarbene  Benzimidazoles  Imidazoles  Pyrazoles
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