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A General Protocol for Cu-Mediated Fluoro-deamination: Sandmeyer Fluorination of Diverse Aromatic Substrates
R Manuel Pérez-García1, Gaute Grønnevik1, Patrick J Riss1
1Section of Organic Chemistry, Department of Chemistry, University of Oslo, Sem Sælands vei 23, 0371 Blindern, Oslo, Norway.
Abstract:
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.
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