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项目整合精选>>>Fluconazole, UK-49858, Zoltec, Loitin, Triflucan, Diflucan
Fluconazole, UK-49858, Zoltec, Loitin, Triflucan, Diflucan
氟康唑Chemical Name: 2-(2,4-Difluorophenyl)-1,3-bis(1H-1,2,4-triazol-1-yl)-2-propanol; alpha-(2,4-Difluorophenyl)-alpha-(1H-1,2,4-triazol-1-ylmethyl)-1H-1,2,4-triazole-1-ethanol; 2,4-Difluoro-alpha,alpha-bis(1H-1,2,4-triazol-1-ylmethyl)benzyl alcohol
CAS No. 86386-73-4
项目整合开发状态: Launched-1988
项目研究机构: Pfizer (Originator), American Pharmaceutical Partners (Not Determined), Vita (Licensee), Sicor (Generic)
合成路线:The Friedel-Crafts' condensation of 1,3-difluorobenzene (I) with chloroacetyl chloride (II) by means of AlCl3 yields alpha-chloro-2,4-difluoroacetophenone (III),which is treated with 1,2,4-triazole (IV) and triethylamine in refluxing ethyl acetate giving alpha-(1H-12,4-triazol-1-yl)-2,4-diftuoroacetophenone (V).The reaction of (V) with trimethylsulfoxonium iodide (VI) by means of NaOH in toluene affords 1-[2-(2,4-di fluorophenyl)-2,3-epoxypropyl]-1H-1,2,4-triazole (VII),which is finally treated again with 1,2,4-triazole (IV) and K2CO3 in hot DMF.
📌 参考资料/链接：
参考文献标题:Triazoles
文献作者:Richardson,K.(Pfizer Inc.)
参考来源:GB 2099818; US 4404216
📄 详细内容
合成路线:The Friedel-Crafts' condensation of 1,3-difluorobenzene (I) with chloroacetyl chloride (II) by means of AlCl3 yields alpha-chloro-2,4-difluoroacetophenone (III),which is treated with 1,2,4-triazole (IV) and triethylamine in refluxing ethyl acetate giving alpha-(1H-12,4-triazol-1-yl)-2,4-diftuoroacetophenone (V).The reaction of (V) with trimethylsulfoxonium iodide (VI) by means of NaOH in toluene affords 1-[2-(2,4-di fluorophenyl)-2,3-epoxypropyl]-1H-1,2,4-triazole (VII),which is finally treated again with 1,2,4-triazole (IV) and K2CO3 in hot DMF.
参考文献标题:Triazole antifungal agents
文献作者:Narayanaswami,S.; Richardson,K.(Pfizer Inc.)
参考来源:EP 0096569; ES 523038
合成路线:The Friedel-Crafts' condensation of 1,3-difluorobenzene (I) with chloroacetyl chloride (II) by means of AlCl3 yields alpha-chloro-2,4-difluoroacetophenone (III),which is treated with 1,2,4-triazole (IV) and triethylamine in refluxing ethyl acetate giving alpha-(1H-12,4-triazol-1-yl)-2,4-diftuoroacetophenone (V).The reaction of (V) with trimethylsulfoxonium iodide (VI) by means of NaOH in toluene affords 1-[2-(2,4-di fluorophenyl)-2,3-epoxypropyl]-1H-1,2,4-triazole (VII),which is finally treated again with 1,2,4-triazole (IV) and K2CO3 in hot DMF.
参考文献标题:Fluconazole
文献作者:Fromtling,R.A.; Castar,J.; Serradell,M.N.
参考来源:Drugs Fut 1985,10(12),982
产品链接: CAS No. 86386-73-4››