Efficient synthesis of 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 nicotinic acetylcholine receptors | Zendy

Zhang Yi | Zendy; Hall Andrew W. | Zendy; Horti Andrew G. | Zendy

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Efficient synthesis of 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 nicotinic acetylcholine receptors

Author(s) -

Zhang Yi,

Hall Andrew W.,

Horti Andrew G.

Publication year - 2004

Publication title -

journal of labelled compounds and radiopharmaceuticals

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.432

H-Index - 47

eISSN - 1099-1344

pISSN - 0362-4803

DOI - 10.1002/jlcr.824

Subject(s) - chemistry , radiosynthesis , radioligand , pyridine , nicotinic agonist , acetylcholine receptor , yield (engineering) , nicotinic acetylcholine receptor , medicinal chemistry , nucleophile , acetylcholine , radiochemistry , nuclear chemistry , receptor , positron emission tomography , organic chemistry , nuclear medicine , biochemistry , pharmacology , medicine , materials science , metallurgy , catalysis

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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