CIESC Journal
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薛叙明,吕春绪
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XUE Xuming,LÜ Chunxu
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摘要: 研究了以4-甲基苯甲醛为原料,经克莱森缩合、N-溴代丁二酰亚胺(NBS)溴化、咪唑缩合以及碱条件下水解反应制得抗血栓药奥扎格雷的工艺。考察了反应物配比、温度控制、NBS用量、缩合反应碱的选择、水解碱用量控制等因素的影响,4步反应总收率为41.6%。
Abstract: :Ozagrel,an anti-thrombosis drug,was synthesized from 4-methylbenzaldehyde by Claisen condensation with ethyl acetate to give ethyl 4-methyl cinnamate,then by bromination with NBS to give ethyl 4-bromomethyl cinnamate,which was condensed with imidazole in alkaline followed by hydrolysis. The optimum process parameters were also determined with an overall yield of 41.6%.
薛叙明,吕春绪. 奥扎格雷合成工艺 [J]. CIESC Journal.
XUE Xuming,LÜ Chunxu. Process for synthesizing ozagrel[J]. .
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https://hgxb.cip.com.cn/CN/Y2009/V28/I11/2024