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【结 构 式】 
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【药物名称】Tibalosin, CP-804-S 【化学名称】1-(2,3-Dihydrobenzo[b]thien-6-yl)-2-(4-phenylbutylamino)propan-1-ol 【CA登记号】63996-84-9 【 分 子 式 】C21H27NOS 【 分 子 量 】341.51944 |
【开发单位】 【药理作用】 |
合成路线1
The Friedel-Crafts' condensation of propionyl chloride (I) with 2,3-dihydrobenzo[b]thiophene (II) in dichloroethylene gives 5-propionyl-2,3-dihydrobenzo[b]thiophene (III), which is brominated with Br2 in THF yielding 5-(2-bromopropionyl)-2,3-dihydrobenzo[b]thiophene (IV). Finally this compound is condensed with 4-phenylbutylamine (V) in refluxing methanol and reduced with NaBH4 in the solvent
| 【1】 Serradell, M.N.; Castaner, J.; Thorpe, P.J.; Tibalosin. Drugs Fut 1984, 9, 12, 909. |
| 【2】 Lambellin, G.; Roba, J.; Gillet, C.; Roncocci, R. (Continental Pharma); BE 848496; FR 2370470; FR 2370472; GB 1565080; JP 7797952 . |
| 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) | 61080 | 2,3-dihydro-1-benzothiophene | C8H8S | 详情 | 详情 | |
| (II) | 15967 | propanoyl chloride; propionyl chloride | 79-03-8 | C3H5ClO | 详情 | 详情 |
| (III) | 61081 | 1-(2,3-dihydro-1-benzothiophen-6-yl)-1-propanone | C11H12OS | 详情 | 详情 | |
| (IV) | 61082 | 2-bromo-1-(2,3-dihydro-1-benzothiophen-6-yl)-1-propanone | C11H11BrOS | 详情 | 详情 | |
| (V) | 37811 | 4-phenyl-1-butanamine; 4-phenylbutylamine | 13214-66-9 | C10H15N | 详情 | 详情 |
Extended Information