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【结 构 式】 
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【药物名称】Etanidazole, NSC-301467, DuP-435, SR-2508, SP-2508, Radinyl 【化学名称】N-(2-Hydroxyethyl)-2-nitroimidazole-1-acetamide 【CA登记号】22668-01-5 【 分 子 式 】C7H10N4O4 【 分 子 量 】214.18215 |
【开发单位】National Cancer Institute (Originator), SRI (Originator), Amersham (Licensee), Roberts (Licensee) 【药理作用】Bladder Cancer Therapy , Oncolytic Drugs, Radiation Therapy, Radiosensitizers |
合成路线1
The condensation of 2-nitroimidazole (I) with methyl chloroacetate (II) by means of sodium methoxide in hot DMF gives methyl (2-nitro-1-imidazolyl)acetate (III), which is then treated with ethanolamine (IV) in methanol.
| 【1】 Castaner, J.; Robinson, C.; Etanidazole. Drugs Fut 1995, 20, 8, 772. |
| 【2】 Lee, W.W.; Brown, J.M.; Martinez, A.P.; Cory, M.J. (US Department of Health & Human Services); Nitroimidazoles of low toxicity and high activity as radiosensitizers of hypoxic tumor cells. US 4371540 . |
| 【3】 Beaman, A.G.; Duschinsky, R.; Tautz, W.P. (F. Hoffmann-La Roche AG); 2-Nitroimidazoles. US 3679698 . |
| 【4】 Beaman, A.G.; Duschinsky, R.; Tautz, W.P. (F. Hoffmann-La Roche AG); Novel imidazole derivs. and a process for the manufacture thereof. GB 1138529 . |
| 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) | 10145 | 2-Nitro-1H-imidazole; 2-Nitroimidazole | 527-73-1 | C3H3N3O2 | 详情 | 详情 |
| (II) | 10257 | methyl 2-chloroacetate; methyl chloroacetate | 96-34-4 | C3H5ClO2 | 详情 | 详情 |
| (III) | 10258 | methyl 2-(2-nitro-1H-imidazol-1-yl)acetate; Methyl 2-nitro-1-imidazoleacetate | 22813-31-6 | C6H7N3O4 | 详情 | 详情 |
| (IV) | 10259 | Ethanol amine;Ethanolamine;2-Aminoethanol; 2-Amino-1-ethanol；2-Aminoethyl alcohol | 141-43-5 | C2H7NO | 详情 | 详情 |
Extended Information