【结 构 式】 |
【分子编号】48611 【品名】N-(2-chloroethyl)-N'-(methylsulfonyl)methanesulfonohydrazide 【CA登记号】 |
【 分 子 式 】C4H11ClN2O4S2 【 分 子 量 】250.72712 【元素组成】C 19.16% H 4.42% Cl 14.14% N 11.17% O 25.52% S 25.58% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号:(III)The reaction of (2-hydroxyethyl)hydrazine (I) with MsCl in pyridine gives the trimesylated compound (II), which is treated with LiCl in refluxing acetone to yield 1-(2-chloroethyl)-1,2-bis(methanesulfonyl)hydrazine (III) (1). Finally, this compound is condensed with methyl isocyanate (IV) by means of TEA in acetonitrile to afford the target semicarbazide.
【1】 Shyam, K.; et al.; Antitumor 2-(aminocarbonyl)-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazines. J Med Chem 1996, 39, 3, 796. |
【2】 Satorelli, A.C.; Shyam, K.; Penketh, P.G. (Yale University); Antitumor 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-(substd.)hydrazines. EP 0841912; JP 1999508898; WO 9702029 . |
【3】 Shyam, K.; et al.; Synthesis and evaluation of 1,2, 2-tris(sulfonyl)hydrazines as antineoplastic and trypanocidal agents. J Med Chem 1990, 33, 8, 2259. |
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) | 24951 | 2-hydrazino-1-ethanol | 109-84-2 | C2H8N2O | 详情 | 详情 |
(II) | 48610 | 2-[1,2-bis(methylsulfonyl)hydrazino]ethyl methanesulfonate | C5H14N2O7S3 | 详情 | 详情 | |
(III) | 48611 | N-(2-chloroethyl)-N'-(methylsulfonyl)methanesulfonohydrazide | C4H11ClN2O4S2 | 详情 | 详情 | |
(IV) | 11019 | (Methylimino)(oxo)methane; methyl isocyanate | C2H3NO | 详情 | 详情 |
Extended Information