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【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