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【结 构 式】 
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【分子编号】59585 【品名】2-[(carboxymethyl)-4-fluoroanilino]-5-chlorobenzoic acid 【CA登记号】 |
【 分 子 式 】C15H11ClFNO4 【 分 子 量 】323.7077832 【元素组成】C 55.66% H 3.43% Cl 10.95% F 5.87% N 4.33% O 19.77% |
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：(VII)In an alternative method, Ullmann arylation of potassium N-(4-fluorophenyl)glycinate (VI) with potassium 2,5-dichlorobenzoate (V) afforded the N,N-diaryl glycine (VII). Cyclization of diacid (VII) in refluxing Ac2O produced the 3-acetoxy indole (VIII). This was then reduced to indole (IV) with NaBH4 in refluxing EtOH.
| 【1】 Perregaard, J.K.; Costall, B. (H. Lundbeck A/S); Piperidyl-substd. indoles. EP 0533824; JP 1993509080; US 5439922; WO 9200070 . |
| 【2】 Bech Sommer, M. (H. Lundbeck A/S); Method of manufacturing sertindole. WO 9851685 . |
| 【3】 Bogeso, K.P.; Hyttel, J.; Sanchez, C.; Arnt, J.; Perregaard, J.; Noncataleptogenic, centrally acting dopamine D-2 and serotonin 5-HT2 antagonists within a series of 3-substituted 1-(4-fluorophenyl)-1H-indoles. J Med Chem 1992, 35, 6, 1092. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (IV) | 59582 | 5-chloro-1-(4-fluorophenyl)-1H-indole | C14H9ClFN | 详情 | 详情 | |
| (V) | 59583 | potassium 2,5-dichlorobenzoate | C7H3Cl2KO2 | 详情 | 详情 | |
| (VI) | 59584 | potassium 2-(4-fluoroanilino)acetate | C8H7FKNO2 | 详情 | 详情 | |
| (VII) | 59585 | 2-[(carboxymethyl)-4-fluoroanilino]-5-chlorobenzoic acid | C15H11ClFNO4 | 详情 | 详情 | |
| (VIII) | 59586 | 5-chloro-1-(4-fluorophenyl)-1H-indol-3-yl acetate | C16H11ClFNO2 | 详情 | 详情 |
Extended Information