✦ LIBER ✦
Synthetic studies with [18F]p-fluorobenzenediazonium chloride application to the synthesis of a radiolabelled glucocorticoid: [18F]WIN 44577
✍ Scribed by Anthony L. Feliu
- Publisher
- John Wiley and Sons
- Year
- 1988
- Tongue
- French
- Weight
- 405 KB
- Volume
- 25
- Category
- Article
- ISSN
- 0022-2135
No coin nor oath required. For personal study only.
✦ Synopsis
A route was devised to synthesize no-carrier-added or carrier-added C*uFlp-fluorophenylhydratine from aqueous C'OFlfluoride. Key reaction in this three-step sequence is the reduction o f C1nFlp-fluorobenzenediazonium chloride with sodium cyanoborohydride. The utility of this method is demonstrated by the synthesis of E'FIWIN 44577, an N-(p-fluoropheny1)pyrazole-containing corticosteroid, which exhibits exceptionally high in vitro binding affinity for type-I1 qlucocorticoid receptors, and which is currently under evaluation as a possible radioligand for positron emission tomographic studies.