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

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.

SUBMITTER: Perez-Garcia RM

PROVIDER: S-EPMC7875512 | biostudies-literature | 2021 Feb

REPOSITORIES: biostudies-literature

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

Pérez-García R Manuel RM Grønnevik Gaute G Riss Patrick J PJ

Organic letters 20210125 3

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 radiosyn ...[more]

PMID: 33492972

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