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

Authors

Maddison Lovell, Sebastiano Ortalli, Raquel Sánchez-Bento, Matthew Tredwell, Joseph Ford, Véronique Gouverneur

Published in

Journal of the American Chemical Society. Jul 03, 2026. Epub Jul 03, 2026.

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 S_N2-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.

PMID:
42397679
Bibliographic data and abstract were imported from PubMed on 03 Jul 2026.

Read full publication at:
Please sign in to see all details.

Stats

1-terrible, 9-excellent. How would you rate this publication? Sign in in to submit your rating.

Post a comment

You need to be signed in to post comments. You can sign in here.

Comments

There are no comments yet.