SNAr Radiofluorination with In Situ Generated [18F]Tetramethylammonium Fluoride.
J Org Chem
; 86(20): 14121-14130, 2021 10 15.
Article
em En
| MEDLINE
| ID: mdl-34505779
ABSTRACT
This report describes a method for the nucleophilic radiofluorination of (hetero)aryl chlorides, (hetero)aryl triflates, and nitroarenes using a combination of [18F]KF·K2.2.2 and Me4NHCO3 for the in situ formation of a strongly nucleophilic fluorinating reagent (proposed to be [18F]Me4NF). This method is applied to 24 substrates bearing diverse functional groups, and it generates [18F](hetero)aryl fluoride products in good to excellent radiochemical yields in the presence of ambient air/moisture. The reaction is applied to the preparation of 18F-labeled HQ-415 for potential (pre)clinical use.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Radioisótopos de Flúor
/
Fluoretos
Idioma:
En
Ano de publicação:
2021
Tipo de documento:
Article