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【结 构 式】 
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【药物名称】DB-51630 【化学名称】3-(5-Nitro-1,3-dioxo-2,3-dihydro-1H-benzo[de]isoquinolin-2-yl)-N-[2-[2-(5-nitro-1,3-dioxo-2,3-dihydro-1H-benzo[de]isoquinolin-2-yl)ethylamino]ethyl]benzamide 【CA登记号】254452-11-4 【 分 子 式 】C35H24N6O9 【 分 子 量 】672.61633 |
【开发单位】Taiho (Originator) 【药理作用】ONCOLYTIC DRUGS, EP300 Expression Enhancers |
合成路线1
The reaction of 3-nitro-1,8-naphthalic anhydride (I) with diethylenetriamine (II) in cool ethanol gives the cyclic monoamide (III). The reaction of the 3-nitro-1,8-naphthalic anhydride (I) with 3-aminobenzoic acid (IV) in hot DMSO/pyridine gives the corresponding cyclic naphthalamide (V). Finally, the benzoic acid (V) is condensed with the amine group of (III) by means of CDI in DMSO to afford the target bis naphthalamide.
| 【1】 Suzuki, K.; Yamada, Y.; Asao, T.; Noguchi, K.; Wakida, M. (Taiho Pharmaceutical Co., Ltd.); Naphthalimidobenzamide derivs.. EP 1020446; US 6300331; WO 0001672 . |
| 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) | 15864 | 5-nitro-1H,3H-benzo[de]isochromene-1,3-dione; 3-Nitro-1,8-naphthalic anhydride | 3027-38-1 | C12H5NO5 | 详情 | 详情 |
| (II) | 55379 | 2,2'-Diaminodiethylamine; 2,2'-Iminodiethylamine; Bis(beta-Aminoethyl)amine; Diethylentriamine; N-(2-Aminoethyl)-1,2-ethanediamine | 111-40-0 | C4H13N3 | 详情 | 详情 |
| (III) | 55424 | 2-{2-[(2-aminoethyl)amino]ethyl}-5-nitro-1H-benzo[de]isoquinoline-1,3(2H)-dione | C16H16N4O4 | 详情 | 详情 | |
| (IV) | 26638 | 3-Aminobenzoic acid | 99-05-8 | C7H7NO2 | 详情 | 详情 |
| (V) | 55382 | 3-[5-nitro-1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl]benzoic acid | C19H10N2O6 | 详情 | 详情 |
Extended Information