2-(5-甲基-2-苯基-4-噁唑)-乙醇的合成  

Synthesis of ethyl 2-(5-methyl-2-phenyl-4-oxazolyl)ethanol

作　　者：蔡小华[1] 胡薇[2] 

机构地区：[1]怀化医学高等专科学校药学系,湖南怀化418000 [2]南昌大学分析测试中心,江西南昌310000

出　　处：《中国药物化学杂志》2004年第4期245-246,共2页Chinese Journal of Medicinal Chemistry

基　　金：湖南省教育厅科研资助项目 (0 2C0 5 0 )

摘　　要：以丙酰乙酸乙酯为起始原料 ,先溴化得到 4 溴丙酰乙酸乙酯 ,再在甲苯中与苯甲酰胺回流环合得到 2 (5 甲基 2 苯基 4 唑 ) 乙酸乙酯 ,最后经氢化铝锂还原 ,得到目标杂环中间体 2 (5 甲基 2 苯基 4 唑 ) 乙醇。该合成方法反应步骤少 ,原料便宜 ,目标物的总收率为 6 7 3%。An important hetercycle intermediate for PPAR agonist ligand 2-(5-methyl-2-phenyl-4-oxazolyl)ethanol was synthesized.It was started from ethyl 3-oxopentanoate,and was brominated,and then ethyl 4-bromo-3-oxopentanoate was produced,which cyclized with benzamide at reflux in toluene and afforded to ethyl 2-(5-methyl-2-phenyl-4-oxazolyl)acetate,then was reduced with lithium aluminum hydride and 2-(5-methyl-2-phenyl-4-oxazolyl)ethanol was gained.The advantage of this synthetic method are shorter reattion steps,cheaper materials an a high total yield with 67.3%.

关 键 词：药物化学 工艺改进 化学合成 丙酰乙酸乙酯 4-溴丙酰乙酸乙酯 2-(5-甲基-2-苯基-4-噁唑)-乙酸乙酯 2-(5-甲基-2-苯基-4-噁唑)-乙醇 

分 类 号：R914.5[医药卫生—药物化学]