药物详细合成路线
| Name | Latoconazole;Lanoconazole;TJN-318;NND-318;Astat | | Chemical Name | (±)-(E)-alpha-[4-(2-Chlorophenyl)-1,3-dithiolan-2-ylidene]-1H-imidazole-1-acetonitrile | | CAS | 101530-10-3 | | Related CAS | | | Formula | C14H10ClN3S2 | | Structure |  | | Formula Weight | 319.8369 | | Stage | 撤市 | | Company | Nihon Nohyaku (Originator), Tsumura (Licensee) | | Activity/Mechanism | Antifungal Agents, ANTIINFECTIVE THERAPY | | Syn. Route | 1 | | Route 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. | | |  | | List of intermediates | No. | | 2-[[(2-amino-5-methoxyphenyl)sulfanyl]methyl]-2-ethylhexanoic acid | (i) | | 3-butyl-3-ethyl-8-methoxy-2,3-dihydro-1,5-benzothiazepin-4(5h)-one | (ii) | | 7-bromo-3-butyl-3-ethyl-8-methoxy-2,3-dihydro-1,5-benzothiazepin-4(5h)-one | (iii) | | | Reference 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 . Reference 2: seo, a.; sugano, h.; hasegawa, c.; ikeda, k.; munechica, y.; konoe, t.; konaka, m. (nihon nohyaku co., ltd.); antifungal agent. jp 1987093227 . Reference 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 . Reference 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 . Reference 5: seo, a.; sugano, h.; hasegawa, c.; miyashiro, y.; nishimura, a.; ikeda, k. (nihon nohyaku co., ltd.); ketene s,s-acetals. jp 1985218387 . Reference 6: castaner, j.; prous, j.; lanoconazole. drugs fut 1993, 18, 3, 222. |
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来源:药化网
作者:药化小编
摘要:本文合成路线介绍的是药物中文名拉诺康唑；英文名Latoconazole;Lanoconazole;TJN-318;NND-318;Astat；CAS[101530-10-3]
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