Nufenoxole, Sc-27166
奴芬克索Chemical Name: 2-[3,3-Diphenyl-3-(2-methyl-1,3,4-oxadiazol-5-yl)propyl]-2-azabicyclo[2.2.2]octane; 2-[3-(5-Methyl-1,3,4-oxadiazol-2-yl)-3,3-diphenylpropyl]-2-azabicyclo[2.2.2]octane
CAS No. 57726-65-5
项目整合开发状态: Phase III
项目研究机构: Ono (Originator), Pfizer (Originator)
合成路线:The reaction of N-(2-chloroethyl)-2-azabicyclo[2.2.2]octane (I) with diphenylacetonitrile (II) by means of KOH in refluxing methyl ethyl ketone gives 4-[2-azabicyclo[2.2.2]octan-2-yl]-2,2-diphenylbutyronitrile (III),which by reaction with NaN3 in DMF at 125 C is converted into 5-[1,1-diphenyl-3-(2-azabicyclo[2.2.2]octan-2-yl)propyl]-1H-tetrazole (IV).Finally,this compound is treated with refluxing acetic anhydride.
📌 参考资料/链接：
参考文献标题:1,1-Diaryl-1-oxadiazolalkylamines
文献作者:Adelstein,G.W.(Pharmacia Corp.)
参考来源:DE 2514183; DE 2514229; FR 2265367; FR 2265376; GB 1456943; GB 1494943; JP 50135081; JP 50135086; US 3917615
📄 详细内容
合成路线:The reaction of N-(2-chloroethyl)-2-azabicyclo[2.2.2]octane (I) with diphenylacetonitrile (II) by means of KOH in refluxing methyl ethyl ketone gives 4-[2-azabicyclo[2.2.2]octan-2-yl]-2,2-diphenylbutyronitrile (III),which by reaction with NaN3 in DMF at 125 C is converted into 5-[1,1-diphenyl-3-(2-azabicyclo[2.2.2]octan-2-yl)propyl]-1H-tetrazole (IV).Finally,this compound is treated with refluxing acetic anhydride.
参考文献标题:Nufenoxole
文献作者:Castar,J.; Hillier,K.
参考来源:Drugs Fut 1978,3(7),533
合成路线:The reaction of N-(2-chloroethyl)-2-azabicyclo[2.2.2]octane (I) with diphenylacetonitrile (II) by means of KOH in refluxing methyl ethyl ketone gives 4-[2-azabicyclo[2.2.2]octan-2-yl]-2,2-diphenylbutyronitrile (III),which by reaction with NaN3 in DMF at 125 C is converted into 5-[1,1-diphenyl-3-(2-azabicyclo[2.2.2]octan-2-yl)propyl]-1H-tetrazole (IV).Finally,this compound is treated with refluxing acetic anhydride.
参考文献标题:3,3-Diphenyl-3-(2-alkyl-1,3,4-ozadiazol-5-yl)propylcycloalkylamine,a novel series of antidiarrheal agents
文献作者:Adelstein,G.W.; Yen,C.H.; Dajani,E.Z.; Bianchi,R.G.
参考来源:J Med Chem 1976,19(10),1221-25
产品链接: CAS No. 57726-65-5››