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- W2000976204 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" @default.
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- W2000976204 date "1995-08-01" @default.
- W2000976204 modified "2023-10-18" @default.
- W2000976204 title "Rapid synthesis of [18F]SR46349B, a potent and selective 5-HT2 receptor antagonist" @default.
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- W2000976204 doi "https://doi.org/10.1002/jlcr.2580360803" @default.
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