Copper-catalyzed cross-coupling improves regioselectivity in creating trifluoromethyl scaffolds, aiding drug discovery.
Given the significance of propargyl trifluoromethyl scaffolds in drug discovery, the development of efficient synthetic approaches for their construction remains a pressing challenge. In this work, we present copper-catalyzed Sonogashira-type cross-coupling between trifluoroalkyl bromides and alkynes. This reaction proceeds under mild conditions with excellent regioselectivity, exhibits broad functional group tolerance across both aryl- and alkyl-substituted derivatives, and provides a practical and efficient approach for the synthesis of CF₃-incorporated alkynes.
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Yu et al. (2025) studied this question.
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