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【结 构 式】 
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【分子编号】56493 【品名】N-[4-(difluoromethoxy)phenyl]acetamide 【CA登记号】 |
【 分 子 式 】C9H9F2NO2 【 分 子 量 】201.1728064 【元素组成】C 53.73% H 4.51% F 18.89% N 6.96% O 15.91% |
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：(I)The precursor 5-(difluoromethoxy)-2-mercaptobenzimidazole (V) was prepared by the following route. Nitration of N-(p-difluoromethoxyphenyl)acetamide (I) provided nitro anilide (II), which was hydrolyzed to the corresponding nitro aniline (III) employing methanolic NaOMe. Reduction of (III) to the phenylenediamine (IV) was performed by catalytic hydrogenation over Pd/C. Then, cyclization of diamine (IV) with potassium O-ethyl dithiocarbonate gave rise to the benzimidazole (V).
| 【1】 Kohl, B.; Sturm, E.; Klemm, K.; Riedel, R.; Figala, V.; Rainer, G.; Schaefer, H.; Senn-Bilfinger, J. (Altana Pharma Deutschland GmbH ); Dialkoxypyridines, process for their preparation, their use and medicines containing them. AU 8543640; EP 0166287; JP 1986022079; US 4758579 . |
| 【2】 Rainer, G.; Riedel, R.; Senn-Bilfinger, J.; Klemm, K.; Schaefer, H.; Figala, V. (Altana Pharma Deutschland GmbH ); Antisecretory substd. pyridylmethylthio-(or sulfinyl)benzimidazoles. EP 0134400; JP 1984206379; JP 1993086037; US 4555518 . |
| 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) | 56493 | N-[4-(difluoromethoxy)phenyl]acetamide | C9H9F2NO2 | 详情 | 详情 | |
| (II) | 56494 | N-[4-(difluoromethoxy)-2-nitrophenyl]acetamide | C9H8F2N2O4 | 详情 | 详情 | |
| (III) | 56495 | 4-(difluoromethoxy)-2-nitroaniline; 4-(difluoromethoxy)-2-nitrophenylamine | C7H6F2N2O3 | 详情 | 详情 | |
| (IV) | 14033 | 4-(Difluoromethoxy)-1,2-benzenediamine; 2-Amino-4-(difluoromethoxy)phenylamine | C7H8F2N2O | 详情 | 详情 | |
| (V) | 14034 | 5-(Difluoromethoxy)-1H-benzimidazole-2-thiol; 5-(Difluoromethoxy)-1H-benzimidazol-2-ylhydrosulfide; 5-Difluoromethoxy-2-mercapto-1H-benzimidazole | 97963-62-7 | C8H6F2N2OS | 详情 | 详情 |
Extended Information