| 依折麦布中间体的合成工艺研究 |
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| 引用本文： | 蔡金刚,赵世明,罗振福,肖如亭. 依折麦布中间体的合成工艺研究[J]. 精细化工中间体, 2011, 41(4): 37-39 |
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| 作者姓名： | 蔡金刚 赵世明 罗振福 肖如亭 |
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| 作者单位： | 1. 天津理工大学化学化工学院,天津,300191
2. 天津药物研究院化学制药部,天津,300193 |
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| 摘 要： | 以氟苯和戊二酸酐为起始原料,经傅-克反应、羰基保护、水解、酰胺化、偶联反应,合成了依折麦布(Ezetimibe)的重要中间体(S)-3-{4-[2-(4-氟苯基)-[1,3]-二氧杂环戊烷-2-基]-丁酰}-4-苯基-噁唑烷-2-酮(1),总收率36.7%,该工艺反应条件温和、原料价廉易得、收率较高,具有工业化前景。
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| 关 键 词： | 依折麦布 依折麦布 中间体 合成 |
Synthesis of the Intermediate of Ezetimibe |
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| CAI Jin-gang,ZHA Shi-min,LUO Zhen-fu,XIA Ru-ting. Synthesis of the Intermediate of Ezetimibe[J]. Fine Chemical Intermediates, 2011, 41(4): 37-39 |
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| Authors: | CAI Jin-gang ZHA Shi-min LUO Zhen-fu XIA Ru-ting |
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| Affiliation: | CAI Jin-gang1,ZHAO Shi-min2*,LUO Zhen-fu2,XIAO Ru-ting1(1.Dept of Chemistry and Chemical Engineering,Tianjin University of Technology,Tianjin 300191,China,2.Centre for Chemical Pharmaceutical Research,Tianjin Institute of Pharmaceutical Research,Tianjin 300193,China) |
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| Abstract: | (S)-3-{4-(2-(4-FluorophenyL)-dioxolane-2-yl]-butyril)-4 phenyl-oxazolidine-2-one(1) is a key intermediate for the preparation of Ezetimibe.1 was synthesized starting from fluorobenzene and glutaric anhydride,via Friedel-crafts alkylation,carbonyl protection,hydrolysis,amidation and coupling,in overall yield of 36.7%.The results showed that this synthetic route is suitable for industrial production with advantages of low cost,mild reaction conditions,and high yield. |
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| Keywords: | ezetimibe ezetimibe intermediate synthesis |
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