| 4-(4-甲氧基苄基氧基)苯丙二酸-4-甲氧基苄基单酯的工艺改进 |
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| 引用本文： | 刘相奎,胡志,袁哲东. 4-(4-甲氧基苄基氧基)苯丙二酸-4-甲氧基苄基单酯的工艺改进[J]. 中国抗生素杂志, 2011, 36(7) |
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| 作者姓名： | 刘相奎 胡志 袁哲东 |
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| 作者单位： | 上海医药工业研究院，创新药物与制药工艺国家重点实验室，上海200437 |
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| 基金项目： | 国家“重大新药创制”科技重大专项 |
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| 摘 要： | 目的 4-(4-甲氧基苄基氧基)苯丙二酸-4-甲氧基苄基单酯的合成工艺改进。方法 以对甲氧基苄醇与盐酸反应后生成的对甲氧基苄氯和对羟基苯乙酸为原料，经过酯化和醚化反应及羧基的α位发生羧基化反应得到4-(4-甲氧基苄基氧基)苯丙二酸-4-甲氧基苄基单酯。结果 目标产物的结构经过熔点，1H-NMR确认。结论 与原工艺相比，改进后的工艺减少了碘化钠的用量，提高了溶剂利用率，收率高，成本低，操作简单。
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| 关 键 词： | 拉氧头孢二钠 中间体 合成 |
Improved progress of 4-(4-methoxybenzyloxy)-phenylmalonic acid-4-methoxybenzyl mono-ester |
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| Liu Xiang-kui,Hu Zhi,Yuan Zhe-dong. Improved progress of 4-(4-methoxybenzyloxy)-phenylmalonic acid-4-methoxybenzyl mono-ester[J]. Chinese Journal of Antibiotics, 2011, 36(7) |
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| Authors: | Liu Xiang-kui Hu Zhi Yuan Zhe-dong |
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| Affiliation: | Liu Xiang-kui,Hu Zhi and Yuan Zhe-dong(Shanghai Institute of Pharmaceutical Industry,State Key Laboratory of New Drug and Pharmaceutical Processes,Shanghai 200437) |
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| Abstract: | Objective To improve the process of 4-(4-methoxybenzyloxy)-phenylmalonic acid-4-methoxybenzyl mono-ester.Methods 4-(4-methoxybenzyloxy)-phenylmalonic acid-4-methoxybenzyl mono-ester was synthesized from the main material 4-methoxybenzyl chloride and 4-hydroxyphenylacetic acid by esterification,etherification and carboxylation.Results The structure of final product was confirmed by 1H-NMR.Conclusion compared with original process,the improved process reduces the amount of sodium iodide and improves the utili... |
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| Keywords: | Latamoxef disodium Intermediate Synthesis |
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