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【结 构 式】

【药物名称】TK-117

【化学名称】3-(3',4'-Methylenedioxybenzoyl)-2'-deoxy-5-fluoro-uridine

【CA登记号】74234-11-0

【 分 子 式 】C17H15FN2O8

【 分 子 量 】394.3161

【开发单位】Toyama (Originator)

【药理作用】ONCOLYTIC DRUGS

合成路线1

The acylation of 3',5'-di-O-(chloroacetyl)-5-fluoro-2'-deoxyuridine (I) with 3,4-methylenedioxybenzoyl chloride (II) by means of triethylamine in dichloromethane gives 3',5'-di-O-(chloroacetyl)-3-(3,4-methylenedioxybenzoyl)-2'-deoxy-5-fluorouridine (III), which is then hydrolyzed with triethylamine in methanol-THF.

1 Terashima, N.; Kitayama, I.; Yamaguchi, T.; Hiraiwa, T.; Omori, M.; Senoura, M.; Yotsuji, M.; Kodama, T.; Kodama, Y.; Aoyama, H. (Toyama Chemical Co., Ltd.); 5-Fluoro-(beta-uridine or 2'-deoxy-beta-uridine) derivatives, a process for producing the same and a carcinostatic agent containing the same. DE 2923368 .
2 Castaner, J.; Castaner, R.M.; Hoshi, A.; Serradell, M.N.; TK-117. Drugs Fut 1987, 12, 9, 865.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 28820 [(2R,3S,5R)-3-[(2-chloroacetyl)oxy]-5-[5-fluoro-2,4-dioxo-3,4-dihydro-1(2H)-pyrimidinyl]tetrahydro-2-furanyl]methyl 2-chloroacetate C13H13Cl2FN2O7 详情 详情
(II) 28821 1,3-benzodioxole-5-carbonyl chloride 20850-43-5 C8H5ClO3 详情 详情
(III) 28822 (2R,3S,5R)-5-[3-(1,3-benzodioxol-5-ylcarbonyl)-5-fluoro-2,4-dioxo-3,4-dihydro-1(2H)-pyrimidinyl]-2-[[(2-chloroacetyl)oxy]methyl]tetrahydro-3-furanyl 2-chloroacetate C21H17Cl2FN2O10 详情 详情
Extended Information