Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 58, Issue 41, Pages 14615-14619Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201906672
Keywords
late-stage C-H functionalization; photoredox catalysis; site selectivity; sulfonium salts; trifluoromethylation
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Incorporation of the CF3 group into arenes has found increasing importance in drug discovery. Herein, we report the first photoredox-catalyzed cross-coupling of aryl thianthrenium salts with a copper-based trifluoromethyl reagent, which enables a site-selective late-stage trifluoromethylation of arenes. The reaction proceeds with broad functional group tolerance, even for complex small molecules on gram scale. The method was further extended to produce pentafluoroethylated derivatives.
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