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搜狐彩票开奖公告查询:Luliconazole, PR-2699, NND-502,187164-19-8,C14-H9-Cl2-N3-S2,

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摘 要:Luliconazole, PR-2699, NND-502,187164-19-8,C14-H9-Cl2-N3-S2,(-)-(R)-(E)-2-[4-(2,4-Dichlorophenyl)-1,3-dithiolan-2-ylidene]-2-(1-imidazolyl)acetonitrile
  • 【藥物名稱】Luliconazole, PR-2699, NND-502
  • 【化學名】(-)-(R)-(E)-2-[4-(2,4-Dichlorophenyl)-1,3-dithiolan-2-ylidene]-2-(1-imidazolyl)acetonitrile
  • 【CAS登記號】187164-19-8
  • 【結構式】Luliconazole, PR-2699, NND-502,187164-19-8,C14-H9-Cl2-N3-S2,--藥物合成數據庫
  • 【分子式】C14-H9-Cl2-N3-S2
  • 【分子量】354.2841
  • 【原研廠家】Nihon Nohyaku (Originator), Bayer (Licensee)
  • 【作用類別】Antifungal Agents, ANTIINFECTIVE THERAPY
  • 【研發狀態】Phase I
  • 【合成情況】 
  • 〖來源〗JP 1997100279; JP 1998158168; US 5900488; WO 9702821
  • 〖合成路線〗
  • 〖標題〗Antifungal agent, cpd. therefor, process for producing the same
  • 〖合成方法〗This compound has been obtained by two similar ways: The enantiocontrolled reduction of 2,4-dichlorophenacyl bromide (I) with BH3/THF and a chiral oxazaborole catalyst gives 1(S)-(2,4-dichlorophenyl)-2-bromoethanol (II), which is treated with Ms-Cl and TEA in dichloromethane to yield the corresponding mesylate (III). Finally, this compound is cyclized with 2-(1-imidazolyl)-3,3-disulfanylacrylonitrile (VI) by means of KOH in DMSO. Alternatively, 1(S)-(2,4-dichlorophenyl)ethane-1,2-diol (VII) is treated with Ms-Cl and TEA in dichloromethane to give the corresponding dimesylate (VIII), which is condensed with the acrylonitrile (VI) with KOH as before. The intermediate acrylonitrile (VI) has been obtained by condensation of 2-(1-imidazolyl)acetonitrile (IV) with CS2 (V) by means of KOH in DMSO.
  • 〖作者〗Kodama, H.; Niwano, Y.; Kanai, K.; Yoshida, M. (Nihon Nohyaku Co., Ltd.)
  • 〖參考〗Kodama, H.; Niwano, Y.; Kanai, K.; Yoshida, M. (Nihon Nohyaku Co., Ltd.); Antifungal agent, cpd. therefor, process for producing the same. JP 1997100279; JP 1998158168; US 5900488; WO 9702821
  • 〖出處〗JP 1997100279; JP 1998158168; US 5900488; WO 9702821,,():
  • 〖備注〗
 
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