New Avenues in Copper-Mediated Trifluoromethylation Reactions Using Fluoroform as the CF3 Source

Organic molecules containing the trifluoromethyl (CF3) group play a vital role in pharmaceuticals, agrochemicals and materials. New trifluoromethylation methods should encompass capabilities to address issues in efficiency, selectivity and CF3 source all at once. Fluoroform (CF3H), an industrial byproduct, has emerged as an attractive CF3 source. The reaction profile of the [CuCF3] reagent derived from fluoroform has surpassed its original applications in cross-coupling type trifluoromethylation. We have discovered a host of unique copper-mediated trifluoromethylation reactions using [CuCF3] from fluoroform, especially under oxidative conditions, to deliver efficient and selective synthesis of trifluoromethylated compounds.