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【结 构 式】 
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【分子编号】24027 【品名】5-(2-[benzyl[2-(2-ethoxyphenoxy)ethyl]amino]propanoyl)-2-methoxybenzenesulfonamide 【CA登记号】 |
【 分 子 式 】C27H32N2O6S 【 分 子 量 】512.62696 【元素组成】C 63.26% H 6.29% N 5.46% O 18.73% S 6.26% |
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：(III)The condensation of 2-methoxy-5-(2-bromopropionyl)benzenesulfonamide (I) with N-benzyl-2-(2 ethoxyphenoxy)ethylamine (II) in refluxing butanone gives the tertiary amine (III), which is reduced with sodium in ethanol to the alcohol (IV). Debenzylation of (IV) with H2 over Pd/C in methanol affords the hydroxyamine (V), which by reaction with SOCl2 in acetonitrile is converted to the corresponding chloro derivative (VI). Finally, this compound is dechlorinated by hydrogenolysis with H2 over Pd/C in methanol.
| 【1】 Niigata, K.; Fujikura, T. (Yamanouchi Pharmaceutical Co., Ltd.); Sulfamoyl-substd. phenethylamine derivs., their preparation, and pharmaceutical compsns., containing them. EP 0034432; US 4373106; US 5447958 . |
| 【2】 Fujikura, T.; et al. (Yamanouchi Pharmaceutical Co., Ltd.); Phenylethanolamine derivatives. DE 2843016; ES 474149; ES 481549; FR 2405931; GB 2006772 . |
| 【3】 Castaner, J.; Mannhold, R.; YM-12617. Drugs Fut 1986, 11, 4, 293. |
| 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) | 24025 | 5-(2-bromopropanoyl)-2-methoxybenzenesulfonamide | C10H12BrNO4S | 详情 | 详情 | |
| (II) | 24026 | N-benzyl-2-(2-ethoxyphenoxy)-1-ethanamine | C17H21NO2 | 详情 | 详情 | |
| (III) | 24027 | 5-(2-[benzyl[2-(2-ethoxyphenoxy)ethyl]amino]propanoyl)-2-methoxybenzenesulfonamide | C27H32N2O6S | 详情 | 详情 | |
| (IV) | 24028 | 5-(2-[benzyl[2-(2-ethoxyphenoxy)ethyl]amino]-1-hydroxypropyl)-2-methoxybenzenesulfonamide | C27H34N2O6S | 详情 | 详情 | |
| (V) | 24029 | 5-(2-[[2-(2-ethoxyphenoxy)ethyl]amino]-1-hydroxypropyl)-2-methoxybenzenesulfonamide | C20H28N2O6S | 详情 | 详情 | |
| (VI) | 24030 | 5-(1-chloro-2-[[2-(2-ethoxyphenoxy)ethyl]amino]propyl)-2-methoxybenzenesulfonamide | C20H27ClN2O5S | 详情 | 详情 |
Extended Information