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We report the synthesis of 18FarylCF3 and 18FarylCHF2 derivatives from arylCF2Br and arylCHFCl precursors applying a silver-mediated halogen exchange with 18Ffluoride. In the absence of Ag(I)OTf, no reaction takes place at room temperature for both classes of substrates; this result demonstrates the beneficial role of silver(I) as a means to induce 18F-incorporation under very mild conditions.
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Véronique Gouverneur
Stefan Verhoog
Lukas Pfeifer
Synlett
University of Oxford
GlaxoSmithKline (United Kingdom)
Advion (United Kingdom)
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Gouverneur et al. (Fri,) studied this question.
www.synapsesocial.com/papers/69dbdb0e50e1971baba3d158 — DOI: https://doi.org/10.1055/s-0035-1560592