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SNAr Radiofluorination with In Situ Generated [18F]Tetramethylammonium Fluoride.
Lee, So Jeong; Morales-Colón, María T; Brooks, Allen F; Wright, Jay S; Makaravage, Katarina J; Scott, Peter J H; Sanford, Melanie S.
Afiliação
  • Lee SJ; Department of Radiology, University of Michigan, Ann Arbor, Michigan 48109, United States.
  • Morales-Colón MT; Gordon Center for Medical Imaging, Department of Radiology, Massachusetts General Hospital, Harvard Medical School, Boston, Massachusetts 02114,United States.
  • Brooks AF; Department of Chemistry, University of Michigan, Ann Arbor, Michigan 48109, United States.
  • Wright JS; Department of Radiology, University of Michigan, Ann Arbor, Michigan 48109, United States.
  • Makaravage KJ; Department of Radiology, University of Michigan, Ann Arbor, Michigan 48109, United States.
  • Scott PJH; Department of Chemistry, University of Michigan, Ann Arbor, Michigan 48109, United States.
  • Sanford MS; Department of Radiology, University of Michigan, Ann Arbor, Michigan 48109, United States.
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.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Radioisótopos de Flúor / Fluoretos Idioma: En Ano de publicação: 2021 Tipo de documento: Article
Texto completo
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XML
PubMed Links
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Radioisótopos de Flúor / Fluoretos Idioma: En Ano de publicação: 2021 Tipo de documento: Article