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

[Image: see text] 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 hig...

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Autores principales: Pérez-García, R. Manuel, Grønnevik, Gaute, Riss, Patrick J.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2021
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7875512/
https://www.ncbi.nlm.nih.gov/pubmed/33492972
http://dx.doi.org/10.1021/acs.orglett.0c04209
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author Pérez-García, R. Manuel
Grønnevik, Gaute
Riss, Patrick J.
author_facet Pérez-García, R. Manuel
Grønnevik, Gaute
Riss, Patrick J.
author_sort Pérez-García, R. Manuel
collection PubMed
description [Image: see text] 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[(18)F]fluorogluthetimide on a radiosynthesis module.
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spelling pubmed-78755122021-02-11 A General Protocol for Cu-Mediated Fluoro-deamination: Sandmeyer Fluorination of Diverse Aromatic Substrates Pérez-García, R. Manuel Grønnevik, Gaute Riss, Patrick J. Org Lett [Image: see text] 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[(18)F]fluorogluthetimide on a radiosynthesis module. American Chemical Society 2021-01-25 2021-02-05 /pmc/articles/PMC7875512/ /pubmed/33492972 http://dx.doi.org/10.1021/acs.orglett.0c04209 Text en © 2021 The Authors. Published by American Chemical Society This is an open access article published under a Creative Commons Attribution (CC-BY) License (http://pubs.acs.org/page/policy/authorchoice_ccby_termsofuse.html) , which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited.
spellingShingle Pérez-García, R. Manuel
Grønnevik, Gaute
Riss, Patrick J.
A General Protocol for Cu-Mediated Fluoro-deamination: Sandmeyer Fluorination of Diverse Aromatic Substrates
title A General Protocol for Cu-Mediated Fluoro-deamination: Sandmeyer Fluorination of Diverse Aromatic Substrates
title_full A General Protocol for Cu-Mediated Fluoro-deamination: Sandmeyer Fluorination of Diverse Aromatic Substrates
title_fullStr A General Protocol for Cu-Mediated Fluoro-deamination: Sandmeyer Fluorination of Diverse Aromatic Substrates
title_full_unstemmed A General Protocol for Cu-Mediated Fluoro-deamination: Sandmeyer Fluorination of Diverse Aromatic Substrates
title_short A General Protocol for Cu-Mediated Fluoro-deamination: Sandmeyer Fluorination of Diverse Aromatic Substrates
title_sort general protocol for cu-mediated fluoro-deamination: sandmeyer fluorination of diverse aromatic substrates
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7875512/
https://www.ncbi.nlm.nih.gov/pubmed/33492972
http://dx.doi.org/10.1021/acs.orglett.0c04209
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