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【结 构 式】 
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【分子编号】47914 【品名】2,3-diaminobenzoic acid 【CA登记号】 |
【 分 子 式 】C7H8N2O2 【 分 子 量 】152.1528 【元素组成】C 55.26% H 5.3% N 18.41% O 21.03% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号：(III)The oxidation of 5-methoxy-1-tetralone (I) with SeO2 gives 5-methoxy-1,2-naphthoquinone (II), which is cyclized with 2,3-diaminobenzoic acid (II) by means of HCl in refluxing ethanol to yield 4-methoxybenzo[a]phenazine-11-carboxylic acid (IV). Finally, this acid is converted into the target amide by its condensation with N1,N1,2(R)-trimethylethane-1,2-diamine (V) by means of CDI in DMF.
| 【1】 Vicker, N.; Burgess, L.; Chuckowree, I.S.; et al.; Novel angular benzophenazines: Dual topoisomerase I and topoisomerase II inhibitors as potential anticancer agents. J Med Chem 2002, 45, 3, 721. |
| 【2】 Vicker, N.; Folkes, A.J.; Wang, S.; Milton, J.; Denny, W.A. (Xenova Group plc); Benzo[a]phenazin-11-carboxamide derivs. and their use as joint inhibitors of topomerase I and II. WO 0146157 . |
| 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) | 18568 | 5-methoxy-3,4-dihydro-1(2H)-naphthalenone | 33892-75-0 | C11H12O2 | 详情 | 详情 |
| (II) | 47913 | 5-methoxy-1,2-naphthalenedione | C11H8O3 | 详情 | 详情 | |
| (III) | 47914 | 2,3-diaminobenzoic acid | C7H8N2O2 | 详情 | 详情 | |
| (IV) | 47915 | 4-methoxybenzo[a]phenazine-11-carboxylic acid | C18H12N2O3 | 详情 | 详情 | |
| (V) | 47916 | (2R)-N(1),N(1)-dimethyl-1,2-propanediamine; N-[(2R)-2-aminopropyl]-N,N-dimethylamine | C5H14N2 | 详情 | 详情 |
Extended Information