A General Protocol for Cu-Mediated Fluoro-deamination: Sandmeyer Fluorination of Diverse Aromatic Substrates

A Cu­(I)-mediated fluoro-deamination method for nucleophilic radiofluorination was devised. The method affords fluorinated aromatic products directly from anilines under both no-carrier added and stoichiometric conditions. Isolated radiochemical yields range from 11% to 81% with high radiochemical p...

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Bibliographic Details
Published in:Organic letters 2021-02, Vol.23 (3), p.1011-1015
Main Authors: Pérez-García, R. Manuel, Grønnevik, Gaute, Riss, Patrick J
Format: Article
Language:English
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Letter
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Summary:A Cu­(I)-mediated fluoro-deamination method for nucleophilic radiofluorination was devised. The method affords fluorinated aromatic products directly from anilines under both no-carrier added and stoichiometric conditions. Isolated radiochemical yields range from 11% to 81% with high radiochemical purities and a molar activity of 58 MBq/nmol. The reaction conditions were implemented successfully in an automated process for production of (S)-4­[18F]­fluorogluthetimide on a radiosynthesis module.
ISSN:1523-7060
1523-7052
DOI:10.1021/acs.orglett.0c04209