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| 2-(5-甲基-2-苯基-4-(口恶)唑)-乙醇的合成 | |
| 引用本文： | 蔡小华,胡薇. 2-(5-甲基-2-苯基-4-(口恶)唑)-乙醇的合成[J]. 中国药物化学杂志, 2004, 14(4): 245-246 |
| 作者姓名： | 蔡小华 胡薇 |
| 作者单位： | 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 |
| 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-(口恶)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-(口恶)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-(口恶)唑)-乙酸乙酯 2-(5-甲基-2-苯基-4-(口恶)唑)-乙醇 |
| 文章编号： | 1005-0108(2004)04-0245-02 |
Synthesis of ethyl 2-(5-methyl-2-phenyl-4-oxazolyl)ethanol |
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| CAI Xiao-hua ,HU Wei. Synthesis of ethyl 2-(5-methyl-2-phenyl-4-oxazolyl)ethanol[J]. Chinese Journal of Medicinal Chemistry, 2004, 14(4): 245-246 | |
| Authors: | CAI Xiao-hua HU Wei |
| Affiliation: | CAI Xiao-hua 1,HU Wei 2 |
| Abstract: | 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%. |
| Keywords: | medicinal chemistry processing improvement chemical synthesis ethyl 3-oxopentanoate ethyl 4-bromo-3-oxopentanoate ethyl 2-(5-methyl-2-phenyl-4-oxazolyl)acetate 2-(5-methyl-2-phenyl-4-oxazolyl)ethanol |
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