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Silver‐Mediated Cycloaddition of Alkynes with CF3CHN2: Highly Regioselective Synthesis of 3‐Trifluoromethylpyrazoles

作者:Feng Li, Jing Nie, Long Sun, Yan Zheng, Jun‐An Ma · 发表于:Angewandte Chemie International Edition · 年份:2013 · DOI:10.1002/anie.201301870 · 被引用次数:187 · 研究领域:Fluorine in Organic Chemistry、Cyclopropane Reaction Mechanisms、Synthesis and Biological Evaluation

Silver screen: The title reaction provides a convenient and efficient method for the construction of 5-substituted 3-trifluoromethylpyrazoles under mild reaction conditions. By using this protocol, the marketed drug Celecoxib (antiarthritic) could be easily synthesized (see scheme; DMF=N,N-dimethylformamide).