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【结 构 式】

【药物名称】Fotemustine, S-10036, Servier-10036, Muphoran

【化学名称】(±)-[1-[3-(2-Chloroethyl)-3-nitrosoureido]ethyl]phosphonic acid diethyl ester

【CA登记号】92118-27-9

【 分 子 式 】C9H19ClN3O5P

【 分 子 量 】315.69568

【开发单位】ADIR (Originator), Servier (Originator), Italfarmaco (Licensee)

【药理作用】Brain Cancer Therapy, Oncolytic Drugs, DNA-Damaging Drugs

合成路线1

The condensation of 2-chloroethyl isocyanate (I) with diethyl 1-aminoethylphosphonate (II) in chloroform gives diethyl 1-[3-(2-chloroethyl)ureido]ethylphosphonate (III), which is then treated with sodium nitrite and formic acid.

1 Lavielle, G.; Cudennec, C. (ADIR et Cie.); New nitrosourea derivs., process for preparing them and pharmaceutical compsns. containing them. FR 2536075 .
2 Prous, J.; Castaner, J.; FOTEMUSTINE < Rec INN >. Drugs Fut 1989, 14, 11, 1042.
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) 11237 1-Chloro-2-isocyanatoethane; 2-Chloroethyl isocyanate 1943-83-5 C3H4ClNO 详情 详情
(II) 19534 diethyl 1-aminoethylphosphonate C6H16NO3P 详情 详情
(III) 19535 diethyl 1-([[(2-chloroethyl)amino]carbonyl]amino)ethylphosphonate C9H20ClN2O4P 详情 详情
Extended Information