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【结 构 式】 
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【药物名称】Azolastone, Mitozolomide, CCRG-81080, NSC-353451, M&B-39565, 46241-RP 【化学名称】3-(2-Chloroethyl)-3,4-dihydro-4-oxoimidazo[5,1-d]-as-tetrazine-8-carboxamide 【CA登记号】85622-95-3 【 分 子 式 】C7H7ClN6O2 【 分 子 量 】242.62584 |
【开发单位】May & Baker (Originator) 【药理作用】Oncolytic Drugs |
合成路线1
By cyclization of 5-diazoimidazole-4-carboxamide (I) with 2-chloroethyl isocyanate (II) in dichloromethane.
| 【1】 Gibson, N.W.; Hickman, J.A.; The role of isocyanates in the toxicity of antitumor haloalkylnitrosoureas. Biochem Pharmacol 1982, 31, 17, 2795-2800. |
| 【2】 Lunt, E.; Stevens, M.F.G.; Stone, R.; Woolbridge, K.R.H. (Cancer Research Campaign Technology Ltd.); Tetrazine derivs., process for their preparation and pharmaceutical compsns. containing them. BE 894175; DE 3231255; FR 2511679; GB 2104522; JP 1983043975; US 5260291 . |
| 【3】 Hopkins, S.J.; Serradell, M.N.; Castaner, J.; Mitozolomide. Drugs Fut 1984, 9, 11, 827. |
| 【4】 Stevens, M.F.G.; Hickman, J.A.; Stone, R.; Gibson, N.W.; Baig, G.U.; Lunt, E.; Newton, C.G.; Antitumor imidazotetrazinones. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3H)-one, a novel broad-spectrum antitumor agent. J Med Chem 1984, 27, 196-201, 196. |
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