✦ LIBER ✦

Synthesis of 6-chloro-3-((2-(S)-azetidinyl)methoxy)-5-(2-[18F]fluoropyridin-4-yl)pyridine ([18F]NIDA 522131), a novel potential radioligand for studying extrathalamic nicotinic acetylcholine receptors by PET

✍ Scribed by Yi Zhang; Andrew G. Horti

Publisher: John Wiley and Sons
Year: 2004
Tongue: French
Weight: 99 KB
Volume: 47
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.883

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✦ Synopsis

Abstract

6‐Chloro‐3‐((2‐(S)‐azetidinyl)methoxy)‐5‐(2‐[^18^F]fluoropyridin‐4‐yl)pyridine ([^18^F]NIDA 522131), a potential radioligand for studying extrathalamic nicotinic acetylcholine receptors by positron‐emission tomography, was synthesized via no‐carrier‐added nucleophilic [^18^F]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 [^18^F]NIDA522131 via corresponding bromo‐derivative 2 is also described. Copyright © 2004 John Wiley & Sons, Ltd.

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