- 作者: 楊憲桂
- 作者服務機構: 成功大學醫學系藥理科
- 中文摘要: The hydrogens at 3-position of diazepam, a frequently prescribed anxiolytic drug worldwide, undergo an efficient exchange with deuterium atoms in alkaline deuterated methanol. The position of deuterium exchange is confirmed by proton nuclear magnetic resonance and mass spectral analyses. A base-catalyzed keto-enol tautomerism is proposed to be responsible for the observed deuterium exchange. This finding has been applied to the preparation of tritium- labeled diazepam in which only aromatic protons are labeled with tritium atoms. A tritium-labeled diazepam lacking tritium atoms at 1 and 3 positions is valuable as a substrate for quantitative metabolism studies.
- 英文摘要: --
- 中文關鍵字: Keto Enol Tautomerism; Diazepam; Deuterium; Tritium Labeling
- 英文關鍵字: 酮烯醇互變異構;二氮平;氘;氚標幟