【药物名称】VNP-40101M, 101M, Cloretazine
化学结构式(Chemical Structure):
参考文献No.32321
标题:Antitumor 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-(substd.)hydrazines
作者:Satorelli, A.C.; Shyam, K.; Penketh, P.G. (Yale University)
来源:EP 0841912; JP 1999508898; WO 9702029
合成路线图解说明:

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.

参考文献No.126651
标题:Synthesis and evaluation of 1,2, 2-tris(sulfonyl)hydrazines as antineoplastic and trypanocidal agents
作者:Shyam, K.; Penketh, P.G.; Divo, A.A.; Loomis, R.H.; Patton, C.L.; Sartorelli, A.C.
来源:J Med Chem 1990,33(8),2259
合成路线图解说明:

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.

参考文献No.366459
标题:Antitumor 2-(aminocarbonyl)-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazines
作者:Shyam, K.; Penketh, P.G.; Loomis, R.H.; Rose, W.C.; Sartorelli, A.C.
来源:J Med Chem 1996,39(3),796
合成路线图解说明:

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.

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