| PPAR激动配体JTT-20993的合成 |
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| 引用本文： | 蔡小华,胡薇.PPAR激动配体JTT-20993的合成[J].中国新药杂志,2004,13(10):912-914. |
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| 作者姓名： | 蔡小华 胡薇 |
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| 作者单位： | 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 |
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| 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-口恶唑基)-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-口恶唑基)-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.
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| 关 键 词： | 丙酰乙酸乙酯 药物合成 糖尿病 降血脂 |
| 文章编号： | 1003-3734(2004)10-0912-03 |
Synthesis of PPAR agonist ligand JTT-20993 |
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| CAI Xiao-Hua,HU Wei.Synthesis of PPAR agonist ligand JTT-20993[J].Chinese Journal of New Drugs,2004,13(10):912-914. |
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| Authors: | CAI Xiao-Hua HU Wei |
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| Abstract: | 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. |
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| Keywords: | JTT-20993 |
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