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【结 构 式】 
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【药物名称】 【化学名称】11-Methoxy-6-[2-(dimethylamino)ethyl]-2-[2-(1-piperidinyl)ethyl]pyrazolo[3,4,5-mn]pyrimido[5,6,1-de]acridine-5,7(2H,6H)-dione 【CA登记号】 【 分 子 式 】C27H32N6O3 【 分 子 量 】488.59449 |
【开发单位】Novuspharma (Originator) 【药理作用】ONCOLYTIC DRUGS, DNA-Intercalating Drugs |
合成路线1
The cyclization of the acridinonecarboxamide (I) with N-[2-(1-piperidinyl)ethyl]hydrazine (II) in 2-ethoxyethanol at 120 C gives the pyrazoloacridine (III) (1), which is cyclized with phosgene (IV) in chloroform at room temperature to afford the target pentacyclic compound.
| 【1】 Antonini, I.; et al.; Synthesis, antitumor cytotoxicity, and DNA-binding of novel N-5,2-Di(omega-aminoalkyl)-2,6-dihydropyrazolo[3,4,5-kl) acridine-5-carboxamides. J Med Chem 2001, 44, 20, 3329. |
| 【2】 Polucci, P.; Pescalli, N.; Menta, E.; Antonini, I.; Gatto, B.; Martelli, S.; Magnano, A.; Palumbo, M.; 2,6-Di(omega-aminoalkyl)-2,5,6,7-tetrahydopyrazolo[3,4,5-mn]pyrimido[5,6,1-de]acridine-5,7-diones: Novel, potent, cytotoxic, and DNA-binding agents. J Med Chem 2002, 45, 3, 696. |
| 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) | 59362 | N-[2-(dimethylamino)ethyl]-7-methoxy-9-oxo-9,10-dihydro-4-acridinecarboxamide | C19H21N3O3 | 详情 | 详情 | |
| (II) | 59363 | 1-(2-hydrazinoethyl)piperidine | C7H17N3 | 详情 | 详情 | |
| (III) | 59364 | N-[2-(dimethylamino)ethyl]-9-methoxy-2-[2-(1-piperidinyl)ethyl]-2,6-dihydropyrazolo[3,4,5-kl]acridine-5-carboxamide | C26H34N6O2 | 详情 | 详情 | |
| (IV) | 56933 | carbonic dichloride | CCl2O | 详情 | 详情 |
Extended Information