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Trifluoromethylation of Heteroarenes via C-H Bond Activation
Baran et al. have reported zinc(II) bis(trifluoromethanesulfinate) dihydrate (1) can be used as a powerful trifluoromethylating reagent for heteroarenes.1-3) 1 is more chemically stable compared with other trifluoromethylating reagents in air and shows high reactivity to heteroarenes. This reaction proceeds via a radical activation of a C-H bond of the heteroarenes. Interestingly, this reaction can be accomplished in water solvent including some impurities such as cell lysate and oolong tea. Thus, 1 is expected to be applied to bioconjugate chemistry.
References
- Practical and innate carbon–hydrogen functionalization of heterocycles
- Preparation and purification of zinc sulfinate reagents for drug discovery
- Radical-Based Regioselective C−H Functionalization of ElectronDeficient Heteroarenes: Scope, Tunability, and Predictability