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Efficient synthesis of 6-chloro-3-((2-(S)-azetidinyl)methoxy)-5-((E)-2-(2-[18F]fluoropyridin-4-yl)vinyl)pyridine ([18F]NIDA 52289), a very high affinity radioligand for nicotinic acetylcholine receptors

✍ Scribed by Yi Zhang; Andrew W. Hall; Andrew G. Horti

Publisher
John Wiley and Sons
Year
2004
Tongue
French
Weight
113 KB
Volume
47
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

6‐Chloro‐3‐((2‐(S)‐azetidinyl)methoxy)‐5‐((E)‐2‐(2‐[^18^F]fluoropyridin‐4‐yl)vinyl)pyridine ([^18^F]NIDA 52289), a very high affinity radioligand for studying nicotinic acetylcholine receptors (nAChRs) by positron‐emission tomography, was synthesized through Kryptofix 222 assisted no‐carrier‐added nucleophilic [^18^F]fluorination of 6‐chloro‐3‐((1‐(tert‐butoxycarbonyl)‐2‐(S)‐azetidinyl)methoxy)‐5‐((E)‐2‐(2‐bromopyridin‐4‐yl)vinyl)pyridine, followed by acidic deprotection. The overall radiochemical yield of the radiosynthesis was 10% (non‐decay‐corrected), the specific radioactivity was in the range of 93–326 GBq/µmol (2.5–8.8 mCi/µmol) and the radiochemical purity was greater than 99%. Copyright © 2004 John Wiley & Sons, Ltd.

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Synthesis of 6-chloro-3-((2-(S)-azetidin
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
✍ Yi Zhang; Andrew G. Horti 📂 Article 📅 2004 🏛 John Wiley and Sons 🌐 French ⚖ 99 KB

## 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]fluorin