Yi Zhang, A. Horti
Nov 1, 2004
Citations
0
Influential Citations
10
Citations
Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
6-Chloro-3-((2-(S)-azetidinyl)methoxy)-5-(2-[18F]fluoropyridin-4-yl)pyridine ([18F]NIDA 522131), a potential radioligand for studying extrathalamic nicotinic acetylcholine receptors by positron-emission tomography, was synthesized via no-carrier-added nucleophilic [18F]fluorination of 6-chloro-3-((1-(tert-butoxycarbonyl)-2-(S)-azetidinyl)methoxy)-5-(2-iodopyridin-4-yl)vinyl)pyridine, followed by acidic deprotection. The overall radiochemical yield of the radiosynthesis was 4–8% (non-decay-corrected), the specific radioactivity was in the range of 167–335 GBq/µmol (4500–9000 mCi/µmol) and the radiochemical purity was greater than 99%. Preparation of [18F]NIDA522131 via corresponding bromo-derivative 2 is also described. Copyright © 2004 John Wiley & Sons, Ltd.