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【结 构 式】

【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