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Updated: Jul 7, 2025

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
Copper Loading-Controlled Selective Synthesis of 2,5-Bis(trifluoromethyl) and Monotrifluoromethyl-Substituted
Wei Wu1, Zipeng Zhang2, Jialong Li1
1Fujian Provincial University Engineering Research Center of Green Materials and Chemical Engineering, and Fujian Engineering Research Center of New Chinese lacquer Material, College of Materials and Chemical Engineering, Minjiang University, Fuzhou 350108, China.
Abstract:
A general domino annulation reaction of sulfonylmethyl isocyanide with trifluoroacetic anhydride in the presence of copper chloride as an additive is developed. The reaction affords 2,5-bis(trifluoromethyl)oxazoles in modest to good yields under mild conditions. A wide variety of sulfonylmethyl isocyanide and perfluorocarboxylic anhydride substrates are amenable to this transformation. Under a higher copper salt loading conditions, the reaction led to the formation of monotrifluoromethyl-substituted oxazole product.
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