SYNTHESIS OF (S)-N-(ENDO-8-METHYL-8-AZABICYCLO[3.2.1] -2-(1-METHYL-2-BUTYNYLOXY)[CARBONYL-C-14]BENZAMIDE MONOHYDROCHLORIDE (C-14-E3620)

Citation
Y. Hoshino et al., SYNTHESIS OF (S)-N-(ENDO-8-METHYL-8-AZABICYCLO[3.2.1] -2-(1-METHYL-2-BUTYNYLOXY)[CARBONYL-C-14]BENZAMIDE MONOHYDROCHLORIDE (C-14-E3620), Journal of labelled compounds & radiopharmaceuticals, 39(2), 1997, pp. 109-114
Citations number
7
Categorie Soggetti
Chemistry Analytical","Pharmacology & Pharmacy","Biochemical Research Methods
ISSN journal
03624803
Volume
39
Issue
2
Year of publication
1997
Pages
109 - 114
Database
ISI
SICI code
0362-4803(1997)39:2<109:SO(->2.0.ZU;2-M
Abstract
(S)-N-(endo-8-Methyl-8-azabicyclo[3.2.1]oct-3 o-2-(1-methyl-2-butnylox y)[carbonyl-C-14]benzamide monohydrochloride (C-14-E3620, 11), which w as required for a study of the pharmacokinetic profile of E3620, is no t only a potent antagonist of 5-HT3 receptors but also a potent agonis t of 5-HT4 receptors. It was synthesized using -chloro-4-(2,5-dimethyl pyrrol-1-yl)-2-(1-methyl-2- butynyloxy)[carboxy-C-14]benzoic acid (8) as the labelled starting material. The product was produced at high ra diochemical purity with a specific activity of 2.02GBq/mmol.