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【结 构 式】 
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【药物名称】Calothrixin A 【化学名称】12,13-Dihydro-7H-indolo[3,2-j]phenanthridine-7,13-dione 5-oxide 【CA登记号】254114-33-5 【 分 子 式 】C19H10N2O3 【 分 子 量 】314.30315 |
【开发单位】Australian National University (Originator) 【药理作用】ANTIINFECTIVE THERAPY, Antimalarials, Oncolytic Drugs, Treatment of Protozoal Diseases |
合成路线1
Methanol derivative (VI) is then condensed with (X) to give pyridazinone derivative (XI) by first mesylation with mesyl chloride (MsCl) and Et3N in dichloromethane followed by condensation with derivative (X) by means of tert-BuOK in DMF in the presence of 18-crown-6. (Alternatively, instead of mesylation, tosylation of (VI) can be performed by treatment with p-toluenesulfonyl chloride in pyridine; in that case, condensation with (X) occurs by means of NaH in DMF).
| 【1】 Kelly, T.R.; et al.; Synthesis of the potent antimalarials calothrixin A and B. Org Lett 2000, 2, 23, 3735. |
| 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) | 46797 | Indole-3-aldehyde; 3-Formylindole; 1H-Indole-3-carbaldehyde; Indole-3-carboxaldehyde | 487-89-8 | C9H7NO | 详情 | 详情 |
| (II) | 46798 | 1-(methoxymethyl)-1H-indole-3-carbaldehyde | C11H11NO2 | 详情 | 详情 | |
| (III) | 45801 | 4-quinolinecarboxylic acid | 486-74-8 | C10H7NO2 | 详情 | 详情 |
| (IV) | 46799 | N,N-diethyl-4-quinolinecarboxamide | C14H16N2O | 详情 | 详情 | |
| (V) | 46800 | 12-(methoxymethyl)-7H-indolo[3,2-j]phenanthridine-7,13(12H)-dione | C21H14N2O3 | 详情 | 详情 | |
| (VI) | 46801 | 7H-indolo[3,2-j]phenanthridine-7,13(12H)-dione | C19H10N2O2 | 详情 | 详情 |