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Herein, we describe a valuable method for the introduction of the (18)FCF3 group into arenes with highly improved specific activity by the reaction of (18)Ftrifluoromethane with aryl iodides or aryl boronic acids. This (18)Ftrifluoromethylation reaction is the first to be described in which the (18)FCF3 products are generated in actual trace amounts and can therefore effectively be used as PET tracers. The method shows broad scope with respect to possible aryl iodide and aryl boronic acid substrates, as well as good to excellent conversion. In particular, the (18)Ftrifluoromethylation of boronic acids was found to outperform (18)Ftrifluoromethylation reactions of halogenated aryl precursors with regard to conversion, reaction conditions, and kinetics.
Born et al. (Tue,) studied this question.