A Ni-Mediated Cross-Coupling Approach to Deuterated 18F- Fluoromethylated (Hetero)arenes

Lovell, Maddison, Ortalli, Sebastiano, Sánchez-Bento, Raquel, Tredwell, Matthew ORCID: https://orcid.org/0000-0002-4184-5611, Ford, Joseph and Gouverneur, Véronique 2026. A Ni-Mediated Cross-Coupling Approach to Deuterated 18F- Fluoromethylated (Hetero)arenes. Journal of the American Chemical Society 148 (27) , pp. 28049-28054. 10.1021/jacs.6c09649

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Abstract

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.

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Schools > Chemistry
Publisher:	American Chemical Society
ISSN:	0002-7863
Date of First Compliant Deposit:	9 July 2026
Last Modified:	06 Aug 2026 08:45
URI:	https://orca.cardiff.ac.uk/id/eprint/188117

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