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Synthesis of 4-fluoro-2, 3-dimethyl-1-phenyl-3-pyrazoline-5-one (4-fluoroantipyrine) and 18f-labeled analog by direct fluorination of antipyrine with molecular fluorine

✍ Scribed by C.-Y. Shiue; A. P. Wolf

Publisher
John Wiley and Sons
Year
1981
Tongue
French
Weight
268 KB
Volume
18
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

A facile procedure for preparing 4‐fluoroantipyrine is reported. Treatment of antipyrine with molecular fluorine gives 4‐fluoroantipyrine (3) and 4,4‐difluoro‐3‐hydroxy‐2,3‐dimethyl‐1‐phenylpyrazolidin‐5‐one (2). The product distribution depends on the ratio of antipyrine and molecular fluorine. The same procedure is used to prepare [^18^F]‐4‐fluoroantipyrine with high specific activity.

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✍ Reeti Katoch-Rouse; Andrew G. Horti 📂 Article 📅 2003 🏛 John Wiley and Sons 🌐 French ⚖ 91 KB

## Abstract The feasibility of nucleophilic displacement of bromide in the 4‐bromopyrazole ring with [^18^F]fluoride has been demonstrated by the synthesis of two radiolabeled compounds: __N__‐(piperidin‐1‐yl)‐5‐(4‐methoxyphenyl)‐1‐(2‐chlorophenyl)‐4‐[^18^F]fluoro‐1__H__‐pyrazole‐3‐carboxamide, ([^