R. Katoch-Rouse, A. Horti
2003
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0
Influential Citations
17
Citations
Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
The feasibility of nucleophilic displacement of bromide in the 4-bromopyrazole ring with [18F]fluoride has been demonstrated by the synthesis of two radiolabeled compounds: N-(piperidin-1-yl)-5-(4-methoxyphenyl)-1-(2-chlorophenyl)-4-[18F]fluoro-1H-pyrazole-3-carboxamide, ([18F] NIDA-42033) 1b and 1-(2-chlorophenyl)-4-[18F]fluoro-5-(4-methoxyphenyl)-1H-pyrazole-3-carboxylic acid, ethyl ester 4. The radiochemical yields were in the range of 1–6%. [18F]NIDA-42033, a potential radiotracer for the study of CB1 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.