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【结 构 式】 
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【分子编号】28936 【品名】N-isopropyl-1-nitroso-2-naphthalenamine 【CA登记号】 |
【 分 子 式 】C13H14N2O 【 分 子 量 】214.26704 【元素组成】C 72.87% H 6.59% N 13.07% O 7.47% |
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：(II)Reaction of 1-nitroso-2-naphthol (I) with isopropylamine in water gives 2-isopropylamino-1-nitrosonaphthalene (II). After hydrogenation, condensation of the resulting 2-isopropylamino-1,2-naphthalendiamine (III) with p-methoxybenzaldehyde yields the 1,2-dihydro derivative (IV), which is converted to MDL-035 with palladium on carbon. Toluene is used as a solvent throughout the synthesis. The overall yield on a 20-kg scale is 57%.
| 【1】 Toja, E.; Schiatti, P.; Selva, D.; 3-Alkyl-2-aryn-3H-naphth[1,2-d]imidazoles, a novel class of nonacidic antiinflammatory agents. J Med Chem 1984, 27, 5, 610-616. |
| 【2】 Toja, E.; Omodei-Sale, A.; Selva, D. (Lepetit SpA); Antimicrobial 3H-naphto[1,2-d]imidazoles. EP 0012866; JP 8092376; US 4340607; US 4435417 . |
| 【3】 Castaner, J.; Chu, S.S.; Serradell, M.N.; Tomoxiprole. Drugs Fut 1985, 10, 2, 133. |
| 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) | 28935 | 1-nitroso-2-naphthol | 131-91-9 | C10H7NO2 | 详情 | 详情 |
| (II) | 28936 | N-isopropyl-1-nitroso-2-naphthalenamine | C13H14N2O | 详情 | 详情 | |
| (III) | 28937 | N-(1-amino-2-naphthyl)-N-isopropylamine | C13H16N2 | 详情 | 详情 | |
| (IV) | 27251 | 4-methoxybenzaldehyde; Anisicaldehyde; p-anisaldehyde | 123-11-5 | C8H8O2 | 详情 | 详情 |
| (V) | 28938 | 3-isopropyl-2-(4-methoxyphenyl)-2,3-dihydro-1H-naphtho[1,2-d]imidazole | C21H22N2O | 详情 | 详情 |
Extended Information