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%. [18]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%.
Original language | English (US) |
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Pages (from-to) | 93-98 |
Number of pages | 6 |
Journal | Journal of Labelled Compounds and Radiopharmaceuticals |
Volume | 46 |
Issue number | 1 |
DOIs | |
State | Published - Jan 2003 |
Externally published | Yes |
Keywords
- Cannabinoid receptors
- F
- Nucleophilic radiofluorination
- Positron emission tomography
- Radiosynthesis
ASJC Scopus subject areas
- Analytical Chemistry
- Biochemistry
- Radiology Nuclear Medicine and imaging
- Drug Discovery
- Spectroscopy
- Organic Chemistry