Expedient Access to 18F-Fluoroheteroarenes via Deaminative Radiofluorination of Aniline-Derived Pyridinium Salts.
Angew Chem Int Ed Engl
; 63(26): e202404945, 2024 Jun 21.
Article
em En
| MEDLINE
| ID: mdl-38624193
ABSTRACT
Herein, we disclose that pyridinium salts derived from abundant (hetero)anilines represent a novel precursor class for nucleophilic aromatic substitution reactions with [18F]fluoride. The value of this new 18F-fluorodeamination is demonstrated with the synthesis of over 30 structurally diverse and complex heteroaryl 18F-fluorides, several derived from scaffolds that were yet to be labelled with fluorine-18. The protocol tolerates heteroarenes and functionalities commonly found in drug discovery libraries, and is amenable to scale-up and automation on a commercial radiosynthesiser.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Compostos de Piridínio
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Sais
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Radioisótopos de Flúor
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Compostos de Anilina
Idioma:
En
Ano de publicação:
2024
Tipo de documento:
Article