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【结 构 式】 
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【药物名称】Pamicogrel, TO-192, KBT-3022, KB-3022, Paminate 【化学名称】2-[4,5-Bis(4-methoxyphenyl)thiazol-2-yl]pyrrole-1-acetic acid ethyl ester 【CA登记号】101001-34-7 【 分 子 式 】C25H24N2O4S 【 分 子 量 】448.54503 |
【开发单位】Kanebo (Originator), Torii (Codevelopment) 【药理作用】Antiplatelet Therapy, Coagulation Disorders Therapy, HEMATOLOGIC DRUGS, Cyclooxygenase Inhibitors |
合成路线1
The cyclization of alpha-bromo-4,4'-dimethoxidesoxybenzoin (I) with pyrrole-2-carbothioamide (II) in hot acetonitrile gives 4,5-bis(4-methoxyphenyl)-2-(pyrrol-2-yl)thiazole (III), which is then condensed with ethyl bromoacetate (IV) by means of NaOH and tetrabutylammonium bromide in refluxing dichloromethane - water.
| 【1】 Yoshino, K.; Seko, N.; Yokota, K.; Ito, K.; Tsukamoto, G. (Kanebo Pharmaceuticals, Ltd.); Novel 4,5-bis(4-methoxyphenyl)-2-(pyrrol-2-yl)thiazoles, process for the preparation thereof and pharmaceutical compsn. containing the same. EP 0159677; JP 1985222481; JP 1986033186; JP 1986200985; US 4659726 . |
| 【2】 Prous, J.; Castaner, J.; KBT-3022. Drugs Fut 1991, 16, 2, 105. |
| 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) | 31235 | 2-bromo-1,2-bis(4-methoxyphenyl)-1-ethanone | C16H15BrO3 | 详情 | 详情 | |
| (II) | 31236 | 1H-pyrrole-2-carbothioamide | C5H6N2S | 详情 | 详情 | |
| (III) | 31237 | 4,5-bis(4-methoxyphenyl)-2-(1H-pyrrol-2-yl)-1,3-thiazole; 4-[4-(4-methoxyphenyl)-2-(1H-pyrrol-2-yl)-1,3-thiazol-5-yl]phenyl methyl ether | C21H18N2O2S | 详情 | 详情 | |
| (IV) | 16640 | Ethyl 2-bromoacetate; Ethyl bromoacetate | 105-36-2 | C4H7BrO2 | 详情 | 详情 |
Extended Information