Synthetic studies with [(18)F]p‐fluorobenzenediazonium chloride: Application to the synthesis of a radiolabelled glucocorticoid: [(18)F]WIN 44577 Journal Article


Author: Feliu, A. L.
Article Title: Synthetic studies with [(18)F]p‐fluorobenzenediazonium chloride: Application to the synthesis of a radiolabelled glucocorticoid: [(18)F]WIN 44577
Abstract: A, route was devised to synthesize no‐carrier‐added or carrier‐added [10F]p‐fluorophenylhydrazine from aqueous [18F]fluoride. Key reaction in this three‐step sequence is the reduction of [18F]p‐fluorobenzenediazonium chloride with sodium cyanoborohydride. The utility of this method is demonstrated by the synthesis of [10F]WIN 44577, an N‐(pfluorophenyl)pyrazole‐containing corticosteroid, which exhibits exceptionally high in vitro binding affinity for type‐II glucocorticoid receptors, and which is currently under evaluation as a possible radioligand for positron emission tomographic studies. Copyright © 1988 John Wiley & Sons, Ltd.
Keywords: unclassified drug; nonhuman; glucocorticoid; radioisotope; synthesis; corticosteroids; diazonium salts; fluorine‐18; p‐fluoroaniline; p‐fluorophenylhydrazine; sodium cyanoborohydride; 4 fluorophenylhydrazine; win 44577
Journal Title: Journal of Labelled Compounds and Radiopharmaceuticals
Volume: 25
Issue: 11
ISSN: 0362-4803
Publisher: Wiley Blackwell  
Date Published: 1988-11-01
Start Page: 1245
End Page: 1254
Language: English
DOI: 10.1002/jlcr.2580251111
PROVIDER: scopus
DOI/URL:
Notes: Article -- Export Date: 6 August 2020 -- Source: Scopus
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  1. Anthony Feliu
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