Galocitabine, Ro-09-1390
加洛他滨Chemical Name: 5'-Deoxy-5-fluoro-N4-(3,4,5-trimethoxybenzoyl)cytidine; N-[1-(5-Deoxy-beta-D-ribofuranosyl)-5-fluoro-2-oxo-1,2-dihydro-4-pyrimidinyl]-3,4,5-trimethoxybenzamide
CAS No. 124012-42-6
项目整合开发状态: Phase II
项目研究机构: Roche (Originator)
合成路线:The silylation of 5'-deoxy-5-fluorocytidine (I) with tert-butyldimethylsilyl chloride and imidazole in DMF gives 2'-O,3'-O-bis(tert-butyldimethylsilyl)-5'-deoxy-5-fluorocytidine (II),which is acylated with 3,4,5-trimethoxybenzoyl chloride (III) and dimethylaminopyridine in dichloromethane to afford 2'-O,3'-O-bis(tert-butyldimethylsilyl)-5'-deoxy-5-fluoro-N4-(3,4,5-trimethoxybenzoyl)cytidine (IV).Finally,this compound is deprotected with tetrabutylammonium fluoride in THF.
📌 参考资料/链接：
参考文献标题:Fluorocytidine derivs.,their preparation and medical preparations containing them
文献作者:Fujiu,M.; Ishitsuka,H.; Miwa,M.; Umeda,I.; Yokose,K.(F.Hoffmann-La Roche AG)
参考来源:AU 8825168; EP 0316704; JP 1989153696; US 4966891
📄 详细内容
合成路线:The silylation of 5'-deoxy-5-fluorocytidine (I) with tert-butyldimethylsilyl chloride and imidazole in DMF gives 2'-O,3'-O-bis(tert-butyldimethylsilyl)-5'-deoxy-5-fluorocytidine (II),which is acylated with 3,4,5-trimethoxybenzoyl chloride (III) and dimethylaminopyridine in dichloromethane to afford 2'-O,3'-O-bis(tert-butyldimethylsilyl)-5'-deoxy-5-fluoro-N4-(3,4,5-trimethoxybenzoyl)cytidine (IV).Finally,this compound is deprotected with tetrabutylammonium fluoride in THF.
参考文献标题:Galocitabine
文献作者:Hoshi,A.; Castar,J.
参考来源:Drugs Fut 1993,18(4),316
产品链接: CAS No. 124012-42-6››