Abstract
Trifluoroethylthio group (SCH2CF3) is a key functionality in several pharmaceutical and agrochemical compounds, the methods for the installation of the 2,2,2-trifluoroethylthio group are sought after. Herein, we report a copper-catalyzed trifluoroethylthiolation reaction of S-(2,2,2-trifluoroethyl) benzenesulfonothioates and phenylboronic acids at room temperature. The reaction achieved the insertion of trifluoroethylthio moiety to efficiently obtain various substituted aryl 2,2,2-trifluoroethyl thioethers in good yields. Mechanistic investigation indicates the trifluoroethylthiolation radical is involved in the catalytic circle. Moreover, trifluoroethylthiolated clofibrate was synthesized in a particular fashion.
Published Version
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