Nucleophilic trifluoromethylation of aryl halides with methyl trifluoroacetate

When associated with an alkaline halide, such as cesium fluoride or cesium chloride, and Cu(I) species, methyl trifluoroacetate (MTFA) constitutes a valuable trifluoromethylating agent for substituting aromatic (or heteroaromatic) iodides and bromides. The reaction can be carried out in DMF at 180 °C or, better, in sulfolane which allows he reaction to proceed at a lower temperature (from 140 °C).

Associated with cesium fluoride or cesium chloride and CuI, methyl trifluoroacetate (MTFA) constitutes a trifluoromethylating agent for substituting aromatic (or heteroaromatic) iodides and bromides.Figure optionsDownload as PowerPoint slide