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【结 构 式】 
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【药物名称】Sepimostat mesilate, TO-187, FUT-187 【化学名称】4-(4,5-Dihydro-1H-imidazol-2-ylamino)benzoic acid 6-amidinonaphthalen-2-yl ester dimethanesulfonate 【CA登记号】103926-82-5, 103926-81-4 (diHCl), 103926-64-3 (free base) 【 分 子 式 】C23H27N5O8S2 【 分 子 量 】565.62834 |
【开发单位】Torii (Originator), Taiho (Licensee) 【药理作用】Esophageal Diseases, Treatment of, Gastroesophageal Reflux Disease, Agents for, GASTROINTESTINAL DRUGS, Complement Inhibitors, Protease Inhibitors |
合成路线1
Esterification of 4-(4,5-dihydro-1H-imidazol-2-ylamino)benzoic acid methanesulfonate (I) with 6-amidino-2-naphthol methanesulfonate (II) by means of dimethylaminopyridine (DMAP) and dicyclohexylcarbodiimide (DCC) in dry pyridine.
| 【1】 Graul, A.; Leeson, P.; Castaner, J.; Sepimostat Mesylate. Drugs Fut 1997, 22, 5, 502. |
| 【2】 Fujii, S.; Okutome, T.; Nakayama, T.; Nunomura, S.; Sudo, K.; Watanabe, S.; Kurumi, M.; Aoyama, T. (Torii Pharmaceutical Co., Ltd.); Novel amidine cpds. AU 8545492; EP 0190356; ES 8607218; US 4777182; US 4820730; WO 8600893 . |
| 【3】 Nakayama, T.; Ikeda, M.; Taira, S.; Ashizawa, H.; Oda, M.; Fujii, S.; Arakawa, K.; Synthesis and structure-activity study of protease inhibitors. V. Chemical modification of 6-amidino-2-naphthyl 4-guanidinobenzoate. Chem Pharm Bull 1993, 41, 1, 117-25. |