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【结 构 式】 
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【分子编号】13705 【品名】diethyl 2-(2,4-dimethoxyphenyl)malonate 【CA登记号】 |
【 分 子 式 】C15H20O6 【 分 子 量 】296.3202 【元素组成】C 60.8% H 6.8% O 32.4% |
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)The cyclization of m-anisidine (I) with 2,4-dimethoxyphenylmalonic acid diethyl ester (II) in refluxing diphenyl ether (270-90 C) gives 3-(2,4-dimethoxyphenyl)-4-hydroxy-7-methoxyquinolin-2-(1H)-one (III), which is submitted to a new cyclization process in refluxing 47% aqueous HBr yielding 3,9-dihydroxybenzofuro[3,2-c]quinolin-6-(5H)-one (IV). Finally, this compound is esterified with N,N-dimethylcarbamoyl chloride (V) by means of triethylamine and dimethylaminopyridine (DMAP) in DMF.
| 【1】 Rabasseda, X.; Castaner, J.; Mealy, N.; KCA-098. Drugs Fut 1995, 20, 3, 235. |
| 【2】 Kamijo, T.; Ujiie, A.; Harada, H.; Tsutsumi, N.; Tsubaki, A.; Yamaguchi, T.; Nagata, H. (Kissei Pharmaceutical Co., Ltd.); Benzofuro[3,2-c]quinoline cpds. AU 8930977; EP 0357172; JP 1990062878; US 5023261 . |
| 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) | 13704 | 3-Methoxyphenylamine; 3-Methoxyaniline; m-Anisidine | 536-90-3 | C7H9NO | 详情 | 详情 |
| (II) | 13705 | diethyl 2-(2,4-dimethoxyphenyl)malonate | C15H20O6 | 详情 | 详情 | |
| (III) | 13706 | 3-(2,4-Dimethoxyphenyl)-4-hydroxy-7-methoxy-2(1H)-quinolinone | C18H17NO5 | 详情 | 详情 | |
| (IV) | 13707 | 3,9-Dihydroxy[1]benzofuro[3,2-c]quinolin-6(5H)-one | C15H9NO4 | 详情 | 详情 | |
| (V) | 13708 | N,N'-Dimethylcarbamoyl chloride; Dimethylcarbamoyl chloride; [(Chlorocarbonyl)(methyl)amino]methane | 79-44-7 | C3H6ClNO | 详情 | 详情 |
Extended Information