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【结 构 式】 
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【药物名称】Latoconazole, Lanoconazole, TJN-318, NND-318, Astat 【化学名称】(±)-(E)-alpha-[4-(2-Chlorophenyl)-1,3-dithiolan-2-ylidene]-1H-imidazole-1-acetonitrile 【CA登记号】101530-10-3 【 分 子 式 】C14H10ClN3S2 【 分 子 量 】319.8369 |
【开发单位】Nihon Nohyaku (Originator), Tsumura (Licensee) 【药理作用】Antifungal Agents, ANTIINFECTIVE THERAPY |
合成路线1
The reaction of 2-(1-imidazolyl)acetonitrile (I) with CS2 and KOH in DMF gives the dithiolate (II), which is then cyclized with 1-(2-chlorophenyl)-1,2-di(methanesulfonyloxy)ethane (III). A column chromatography over silicagel allows the separation of the (E)- and (Z)-isomers.
| 【1】 Seo, A.; Kanno, H.; Hasegawa, N.; Miyagi, Y.; Nishimura, A.; Konaka, S.; Ohmi, T.; Munechika, Y.; Uchida, M.; Ikeda, K. (Nihon Nohyaku Co., Ltd.); A novel ketene S,S-acetal deriv., a process for manufacturing thereof and a method for curing mycosis by administering it. EP 0218736 . |
| 【2】 Seo, A.; Sugano, H.; Hasegawa, C.; Ikeda, K.; Munechica, Y.; Konoe, T.; Konaka, M. (Nihon Nohyaku Co., Ltd.); Antifungal agent. JP 1987093227 . |
| 【3】 Seo, A.; Sugano, H.; Hasegawa, C.; Ikeda, K.; Nishimura, A.; Miyashiro, Y. (Nihon Nohyaku Co., Ltd.); Non-medicinal bactericidal agents and method for their preparation. JP 1987093204 . |
| 【4】 Seo, A.; Kanno, H.; Hasegawa, N.; Miyagi, Y.; Nishimura, A.; Konaka, S.; Ohmi, T.; Munechika, Y.; Uchida, M.; Ikeda, K. (Nihon Nohyaku Co., Ltd.); Antimycotic agent and fungicidal agent. US 4738976 . |
| 【5】 Seo, A.; Sugano, H.; Hasegawa, C.; Miyashiro, Y.; Nishimura, A.; Ikeda, K. (Nihon Nohyaku Co., Ltd.); Ketene S,S-acetals. JP 1985218387 . |
| 【6】 Castaner, J.; Prous, J.; Lanoconazole. Drugs Fut 1993, 18, 3, 222. |
Extended Information