Mofegiline hydrochloride, MDL-72974A
莫非吉兰 莫非吉兰 Chemical Name: (E)-3-Fluoro-2-[2-(4-fluorophenyl)ethyl]allylamine hydrochloride; (E)-4-Fluoro-beta-(fluoromethylene)benzenebutanamine hydrochloride
CAS No. 120635-25-8, 119386-96-8 (free base)
项目整合开发状态: Phase III
项目研究机构: Aventis Pharma (Originator)
合成路线:The key steps in the synthesis of MDL-72,974A were the conversion of (II) to (IV).Treatment of the malonate (II) with sodium tert-butoxide followed by ClCHF2 afforded the difluoromalonate (III),which was selectively deprotected with CF3CO2H,then reacted with base to stereoselectively yield (E)-(IV).Elaboration of (IV) to MDL-72,974A followed standard procedures; the final product was purified via the N-BOC derivative.
📌 参考资料/链接：
参考文献标题:MDL-72,974A
文献作者:McDonald,I.A.; Bey,P.; Zreika,M.; Palfreyman,M.G.
参考来源:Drugs Fut 1991,16(5),428
📄 详细内容
合成路线:The key steps in the synthesis of MDL-72,974A were the conversion of (II) to (IV).Treatment of the malonate (II) with sodium tert-butoxide followed by ClCHF2 afforded the difluoromalonate (III),which was selectively deprotected with CF3CO2H,then reacted with base to stereoselectively yield (E)-(IV).Elaboration of (IV) to MDL-72,974A followed standard procedures; the final product was purified via the N-BOC derivative.
参考文献标题:Enzyme-activated irreversible inhibitors of monoamine oxidase: Phenylallylamine structure-activity relationships
文献作者:McDonald,I.A.; Lacoste,J.M.; Bey,P.; Palfreyman,M.G.; Zreika,M.
参考来源:J Med Chem 1985,28(2),186-93
产品链接: CAS No. 120635-25-8›› 产品链接: CAS No.119386-96-8››