Xamoterol fumarate, TI-31, ICI-118587, Sepan, Corwin
扎莫特罗Chemical Name: (?-1-(p-Hydroxyphenoxy)-3-[2-(morpholinocarbonamido)ethylamino]-2-propanol hemifumarate; (?-N-[2-[[2-Hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]-4-morpholinecarboxamide (E)-2-butenedioate(2:1) (salt)
CAS No. 90730-93-1, 69630-19-9 ((1:1) salt), 81801-12-9 (free base)
项目整合开发状态: Launched-1988
项目研究机构: AstraZeneca (Originator), Stuart Pharma. (Originator), Yamanouchi (Originator)
合成路线:The reaction of 1-(p-benzyloxyphenoxy)-2,3-epoxypropane (I) with 4-[N-(2-aminoethyl)carbamoyl]morpholine (II) by means of KOH in isopropanol gives 1-(p-benzyloxyphenoxy)-3-[2-(morpholinocarbonamido)ethylamino]-2-propanol (III),which is debenzylated by treatment with H2 over Pd/C in ethanol acetic acid and treated with a solution of fumaric acid in ethanol.
📌 参考资料/链接：
参考文献标题:Morpholine carboxamides and use thereof
文献作者:Main,B.G.; Barlow,J.J.(AstraZeneca plc)
参考来源:FR 2391997; JP 53147038; US 4143140; US 4172150
📄 详细内容
合成路线:The reaction of 1-(p-benzyloxyphenoxy)-2,3-epoxypropane (I) with 4-[N-(2-aminoethyl)carbamoyl]morpholine (II) by means of KOH in isopropanol gives 1-(p-benzyloxyphenoxy)-3-[2-(morpholinocarbonamido)ethylamino]-2-propanol (III),which is debenzylated by treatment with H2 over Pd/C in ethanol acetic acid and treated with a solution of fumaric acid in ethanol.
参考文献标题:ICI-118,587
文献作者:Blancafort,P.; Serradell,M.N.; Thorpe,P.J.; Castar,J.
参考来源:Drugs Fut 1982,7(8),571
产品链接: CAS No.81801-12-9››