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Copper(II)-Catalyzed Direct C-H Trifluoroethylation of Heteroarenes.

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Trifluoroethyl (CH2CF3) is an important functional group in many pharmaceutical and agrochemical compounds. Herein, we report an efficient method for the copper-catalyzed direct trifluoroethylation of heteroarenes. The reaction exhibited good… Click to show full abstract

Trifluoroethyl (CH2CF3) is an important functional group in many pharmaceutical and agrochemical compounds. Herein, we report an efficient method for the copper-catalyzed direct trifluoroethylation of heteroarenes. The reaction exhibited good compatibility to various substrates, and the desired products were obtained in good yields. Preliminary mechanistic investigations indicate the trifluoroethyl radical is involved in the catalytic circle. Moreover, the late-stage modification of bioactive molecules further confirmed the practical applications of this method.

Keywords: trifluoroethylation heteroarenes; direct trifluoroethylation; copper catalyzed; catalyzed direct

Journal Title: Organic letters
Year Published: 2022

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