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Novel approach enhances fluoromethylation for PET ligands in diverse substrates, facilitating discovery campaigns.
Herein, we report a Ni-mediated 18F,D2-monofluoromethylation of (hetero)arenes from (pseudo)halide coupling partners. This new approach offers key advantages compared to traditional radiochemistry based on SN2-type reactivity with [18F]fluoride. These include increased precursor stability and availability, obviating bespoke precursor syntheses, broad functional group tolerance, and the late-stage introduction of deuterium and fluorine-18 in a single step, all features facilitating early access to PET ligands for discovery campaigns. This novel protocol is applied to over 30 diverse substrates, including complex bioactive molecules, and is amenable to scale-up via a semiautomated protocol on a commercial platform, illustrated by isolation of a 18F,D2-labeled PARP radiotracer.
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Lovell et al. (2026) studied this question.
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