Galocitabine, Ro-09-1390-药物合成数据库

【药物名称】Galocitabine, Ro-09-1390

化学结构式(Chemical Structure):

参考文献No.	10454
标题:	Fluorocytidine derivs., their preparation and medical preparations containing them
作者:	Fujiu, M.; Ishitsuka, H.; Miwa, M.; Umeda, I.; Yokose, K. (F. Hoffmann-La Roche AG)
来源:	AU 8825168; EP 0316704; JP 1989153696; US 4966891

合成路线图解说明: 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No.	202805
标题:	Galocitabine
作者:	Hoshi, A.; Casta馿r, J.
来源:	Drugs Fut 1993,18(4),316

合成路线图解说明: 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.