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Updated: Mar 19, 2026

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
Accessing CF3-Cyclopropenes ─ A Platform for the Synthesis of Trifluoromethylated Building Blocks
Wei Wu1, Tobias M Milzarek1, Matthew D Wodrich2
1Laboratory of Catalysis and Organic Synthesis, Institute of Chemical Sciences and Engineering, École Polytechnique Fédérale de Lausanne, CH-1015 Lausanne, Switzerland.
None:
Cyclopropenes are the smallest unsaturated carbocycles. They possess exceptionally high ring strain, resulting in unique reactivity, enabling C═C bond functionalization and ring-opening transformations. Herein, we report a copper-mediated trifluoromethylation of cyclopropenyl benziodoxole (CpBX) reagents, providing access to previously inaccessible, yet highly useful, sp2-trifluoromethylated cyclopropenes. Subsequent functionalizations of these novel strained ring building blocks enable access to highly substituted trifluoromethylated cyclopropanes, difluoromethylene cyclopropanes and noncyclic trifluoromethylated compounds.
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