PPAR激动配体JTT-20993的合成  

Synthesis of PPAR agonist ligand JTT-20993

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,怀化418000 [2]南昌大学分析测试中心,南昌330027

出　　处：《中国新药杂志》2004年第10期912-914,共3页Chinese Journal of New Drugs

基　　金：湖南省教育厅科研资助项目(02C050)

摘　　要：目的:合成PPAR激动配体JTT-20993。方法: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,然后与苯甲酰胺回流环合得到2-(5-甲基-2-苯基-4-(？)唑基)-乙酸乙酯,再还原成醇,并甲磺酰化,得到中间体2-(5-甲基-2-苯基-4-(?)唑基)-乙醇甲磺酸酯,最后与4-羟基苄基丙二酸二甲酯缩合,得到目标物JTT-20993。结果:目标物经核磁共振氢谱确证,总收率为56.9％。结论:本法反应步骤少,原料便宜,总收率高,优于文献方法。Objective: To synthesize PPAR agonist ligand JTT20993. Methods: Starting from ethyl 3-oxopentanoate,JTT-20993 was obtained via a series of chemical reactions including bromina tion,cyclization,alcoholization,methanesulfonization and condensation. Results: The structure of JTT-20993 was elucidated by 1H-NMR. The total yield was 56. 9%. Conclusion:This synthetic process is better than the literature's methods in the reacting steps,the cost of raw materials and the yield.

关 键 词：丙酰乙酸乙酯 JTT-20993 药物合成 糖尿病 降血脂 

分 类 号：R914.5[医药卫生—药物化学] R977.15[医药卫生—药学]