Fenticonazole nitrate, Rec-151476B free base, Rec-151476, Lomexin
硝酸芬替康唑 芬替康唑 Chemical Name: (?-1-[2-(2,4-Dichlorophenyl)-2-[[4-(phenylthio)phenyl]methoxy]ethyl]-1H-imidazole mononitrate
CAS No. 73151-29-8, 72479-26-6 (free base)
项目整合开发状态: Launched-1986
项目研究机构: Recordati (Originator), SK Pharma (Not Determined), Effik (Licensee), Gerot (Licensee), Pfizer (Licensee)
合成路线:The reduction of 2,4-dichlorophenacyl chloride with NaBH4 gives 1-(2,4-dichlorophenyl)-2-chloroethanol (II),which is condensed with imidazole (III) to yield 1-(2,4-dichlorophenyl)-2-(N-imidazolyl)ethanol (IV).Finally,this compound is condensed with 4-(phenylthio)benzyl chloride (V) [prepared by chloromethylation of diphenyl sulfide (VI) with formaldehyde and HCl] using NaH as condensing agent.
📌 参考资料/链接:
参考文献标题:Substituted dibenzyl ethers and parmaceutical compositions containing said ethers for the treatment of infections
文献作者:Nardi,D.; Massarani,E.; Tajana,A.; Veronese,M.(Recordati Industria Chimica e Farmaceutica SpA)
参考来源:DE 2917244; FR 2426047; GB 2025395; US 4221803
📄 详细内容
合成路线:The reduction of 2,4-dichlorophenacyl chloride with NaBH4 gives 1-(2,4-dichlorophenyl)-2-chloroethanol (II),which is condensed with imidazole (III) to yield 1-(2,4-dichlorophenyl)-2-(N-imidazolyl)ethanol (IV).Finally,this compound is condensed with 4-(phenylthio)benzyl chloride (V) [prepared by chloromethylation of diphenyl sulfide (VI) with formaldehyde and HCl] using NaH as condensing agent.
参考文献标题:Fenticonazole Nitrate
文献作者:Blancafort,P.; Castar,J.; Serradell,M.N.
参考来源:Drugs Fut 1983,8(9),767
合成路线:The reduction of 2,4-dichlorophenacyl chloride with NaBH4 gives 1-(2,4-dichlorophenyl)-2-chloroethanol (II),which is condensed with imidazole (III) to yield 1-(2,4-dichlorophenyl)-2-(N-imidazolyl)ethanol (IV).Finally,this compound is condensed with 4-(phenylthio)benzyl chloride (V) [prepared by chloromethylation of diphenyl sulfide (VI) with formaldehyde and HCl] using NaH as condensing agent.
参考文献标题:Physico-chemical,structural and analytical studies on fenticonazole,a new drug with antimycotic properties
文献作者:Cova,A.; Tajana,A.; Nardi,D.; Cappelleti,R.; Sibilia,C.
参考来源:Arzneim-Forsch Drug Res 1981,31(12),2127
产品链接: CAS No. 73151-29-8›› 产品链接: CAS No.72479-26-6››