This research reveals a copper-catalyzed process that produces trifluoromethyl amines in various alkenes, suggesting its utility in drug development.
A general copper-catalyzed intermolecular aminotrifluoromethylation of alkenes with free anilines and Togni's reagent is reported. Distinguished by its versatile reactivity, this protocol enables the coupling of diverse primary and secondary anilines ranging from electron-deficient to oxidatively sensitive electron-rich substrates. The reaction features mild conditions and accommodates a wide range of alkenes, including styrenes, α-substituted styrenes, and unactivated alkenes. This method provides a robust platform for accessing β-trifluoromethyl amines, including those with quaternary carbon centers, and is applicable to the late-stage functionalization of pharmaceutical derivatives.
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Yu et al. (2026) studied this question.
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