VNP-40101M, 101M, Cloretazine
1,2-双(甲磺酰基)-1-(2-氯乙基)-2-(甲氨羰基)肼Chemical Name: 1-(2-Chloroethyl)-4-methyl-1,2-bis(methylsulfonyl)semicarbazide
CAS No. 173424-77-6
项目整合开发状态: Phase II
项目研究机构: Vion (Orphan Drug), Yale University (Originator), Vion (Licensee)
合成路线: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.
📌 参考资料/链接：
参考文献标题:Antitumor 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-(substd.)hydrazines
文献作者:Satorelli,A.C.; Shyam,K.; Penketh,P.G.(Yale University)
参考来源:EP 0841912; JP 1999508898; WO 9702029
📄 详细内容
合成路线: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.
参考文献标题:Synthesis and evaluation of 1,2,2-tris(sulfonyl)hydrazines as antineoplastic and trypanocidal agents
文献作者:Shyam,K.; Penketh,P.G.; Divo,A.A.; Loomis,R.H.; Patton,C.L.; Sartorelli,A.C.
参考来源:J Med Chem 1990,33(8),2259
合成路线: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.
参考文献标题:Antitumor 2-(aminocarbonyl)-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazines
文献作者:Shyam,K.; Penketh,P.G.; Loomis,R.H.; Rose,W.C.; Sartorelli,A.C.
参考来源:J Med Chem 1996,39(3),796
产品链接: CAS No. 173424-77-6››