期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 54, 期 22, 页码 6558-6561出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201501529
关键词
alkynes; cycloaddition; difluoromethylation; fluorine; pyrazoles
A novel approach to agrochemically important difluoromethyl-substituted pyrazoles has been developed based on the elusive reagent CF2HCHN2, which was synthesized (generated insitu) for the first time and employed in [3+2]cycloaddition reactions with alkynes. The reaction is extremely practical as it is a one-pot process, does not require a catalyst or the isolation of the potentially toxic and explosive gaseous intermediate, and proceeds in a common solvent, namely chloroform, in air. The reaction is also scalable and allows for the preparation of the target pyrazoles on gram scale.
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