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Synthetic studies with [ 18 F]p‐fluorobenzenediazonium chloride application to the synthesis of a radiolabelled glucocorticoid: [ 18 F]WIN 44577
Author(s) -
Feliu Anthony L.
Publication year - 1988
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580251111
Subject(s) - chemistry , glucocorticoid , chloride , radioligand , sodium , aqueous solution , radiochemistry , stereochemistry , nuclear chemistry , in vitro , organic chemistry , biochemistry , endocrinology , medicine
A, route was devised to synthesize no‐carrier‐added or carrier‐added [ 10 F]p‐fluorophenylhydrazine from aqueous [ 18 F]fluoride. Key reaction in this three‐step sequence is the reduction of [ 18 F]p‐fluorobenzenediazonium chloride with sodium cyanoborohydride. The utility of this method is demonstrated by the synthesis of [ 10 F]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.