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【结 构 式】 
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【分子编号】14097 【品名】5-Chloro-3-[(Z)-(4,5-dibromo-2-thienyl)(hydroxy)methylidene]-2-oxo-1H-indole-1(2H)-carboxamide 【CA登记号】 |
【 分 子 式 】C14H7Br2ClN2O3S 【 分 子 量 】478.54796 【元素组成】C 35.14% H 1.47% Br 33.39% Cl 7.41% N 5.85% O 10.03% S 6.7% |
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：(IV)A new synthesis of tenidap sodium has been described: The reaction of 4,5-dibromothiophene-2-carboxylic acid (I) with hot SOCl2 gives the corresponding acyl chloride (II), which is condensed with 5-chloro-2-oxo-2,3-dihydro-1H-indole-1-carboxamide (III) by means of 4-(dimethylamino)pyridine (DMAP) in DMF, yielding 5-chloro-3-[(4,5-dibromothien-2-yl)hydroxymethylene]-2-oxo-2,3-dihydro-1H-indole-1-carboxamide (IV). Finally, this compound is debrominated by hydrogenation with H2 over Pd/BaSO4 in methanol.
| 【1】 Schulte, G.R.; Ehrgott, F.J. (Pfizer Inc.); 3-Aroyl-2-oxindole-1-carboxamides. EP 0421749; JP 1991151380; US 5059693 . |
| 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) | 14094 | 4,5-Dibromo-2-thiophenecarboxylic acid; 4,5-Dibromothiophene-2-carboxylic acid | 7311-68-4 | C5H2Br2O2S | 详情 | 详情 |
| (II) | 14095 | 4,5-Dibromo-2-thiophenecarbonyl chloride | C5HBr2ClOS | 详情 | 详情 | |
| (III) | 14096 | 5-Chloro-2-oxo-1-indolinecarboxamide | C9H7ClN2O2 | 详情 | 详情 | |
| (IV) | 14097 | 5-Chloro-3-[(Z)-(4,5-dibromo-2-thienyl)(hydroxy)methylidene]-2-oxo-1H-indole-1(2H)-carboxamide | C14H7Br2ClN2O3S | 详情 | 详情 |
Extended Information