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Rapid synthesis of [18F]SR46349B, a potent and selective 5-HT2 receptor antagonist

✍ Scribed by Pingzhong Tan; Joanna S. Fowler; Yu-Shin Ding; David J. Schlyer

Publisher
John Wiley and Sons
Year
1995
Tongue
French
Weight
483 KB
Volume
36
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

F‐18 labeled SR46349B, a highly potent and selective 5‐HT~2~ receptor antagonist, was synthesized as a potential radioligand for PET studies of brain 5‐HT~2~ receptors. Nucleophilic aromatic substitution of trans‐1‐(2‐nitrophenyl)‐3‐(4‐methoxymethoxyphenyl)‐2‐propenone (10) with NCA [^18^F]fluoride in the presence of potassium carbonate and kryptofix‐222, followed by HCl hydrolysis, gave F‐18 labeled 12, which was purified by a novel combination of C‐18 Sep‐Pak and silica column chromatography. Subsequent condensation of [^18^F]ketone 12 with Me~2~NCH~2~CH~2~ONH~2~ gave a mixture of [^18^F]SR46349B and its geometric isomer, which was separated by high performance liquid chromatography. The three step hot synthesis of [^18^F]SR46349B required 170 min. and gave a specific activity of 1140 Ci/mmol, 5% radiochemical yield (EOB) and 96% radiochemical purity.

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