✦ LIBER ✦

Synthesis of N-(piperidin-1-yl)-5-(4-methoxyphenyl)-1-(2-chlorophenyl)-4-[18F]fluoro-1H-pyrazole-3-carboxamide by nucleophilic [18F] fluorination: a PET radiotracer for studying CB1 cannabinoid receptors

✍ Scribed by Reeti Katoch-Rouse; Andrew G. Horti

Publisher: John Wiley and Sons
Year: 2003
Tongue: French
Weight: 91 KB
Volume: 46
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.647

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✦ Synopsis

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, ([^18^F] NIDA‐42033) 1b and 1‐(2‐chlorophenyl)‐4‐[^18^F]fluoro‐5‐(4‐methoxyphenyl)‐1__H__‐pyrazole‐3‐carboxylic acid, ethyl ester 4. The radiochemical yields were in the range of 1–6%. [^18^F]NIDA‐42033, a potential radiotracer for the study of CB~1~ cannabinoid receptors in the animal brain by positron emission tomography, has been synthesized in sufficient quantities with specific radioactivity greater than 2500 mCi/μmol and radiochemical purity >95%. Copyright © 2002 John Wiley & Sons, Ltd.

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