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Updated: May 24, 2025

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
Copper-Mediated Direct Trifluoromethylation of Trichloromethyl Alkanes
Ziming Wu1,2, Zehai Lu2, Yongrui Luo2
1Key Laboratory of Structure-Based Drugs Design and Discovery (Ministry of Education), School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016 China.
Abstract:
CF3CCl2-containing compounds are of significant synthetic value but are typically synthesized from environmentally harmful hydrochlorofluorocarbons (CFCs). Herein, we report the use of a well-defined Cu(I) complex, [(bpy)Cu(CF3)], as an efficient trifluoromethylating reagent for the direct trifluoromethylation of trichloroalkanes under mild conditions, affording CF3CCl2-containing products with excellent chemoselectivity. This protocol also enabled the gram-scale synthesis of cyhalothric acid ester, which is a key intermediate in the production of pyrethroid pesticides.
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