Synthetic studies with [18F]p‐fluorobenzenediazonium chloride application to the synthesis of a radiolabelled glucocorticoid: [18F]WIN 44577

Abstract

AbstractA, 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.