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半合成青霉素类抗生素阿扑西林的合成改进
Improved synthesis of aspoxicillin,a semi-synthetic penicillin
【摘要】 目的:优化半合成青霉素类抗生素阿扑西林的合成路线。方法:以D-天门冬氨酸和阿莫西林三水酸为原料,经过6步反应形成产物。结果:经过IR,1H-NMR和13C-NMR分析,证明产物是阿扑西林。结论:本方法原料易得,反应条件温和,成本低,易于放大生产。
【Abstract】 Objective:To optimize the synthetic route of aspoxicillin,a semi-synthetic penicillin. Methods:Aspoxicillin was prepared by a 6-step process using D-aspartic acid and amoxicillin trihydrate as the starting materials. Results:The chemical structure of aspoxicillin was verified by IR,1H-NMR and 13C-NMR. Conclusion:The reported process for the synthesis of aspoxicillin has the advantages such as readily available starting materials,mild reaction conditions,low cost and easily scaled-up capability.
【关键词】 阿扑西林;
半合成青霉素;
D-天门冬氨酸;
阿莫西林三水酸;
【Key words】 aspoxicillin; semisynthetic penicillin; D-aspartic acid; amoxicillin trihydrate;
【Key words】 aspoxicillin; semisynthetic penicillin; D-aspartic acid; amoxicillin trihydrate;
- 【文献出处】 中国新药杂志 ,Chinese Journal of New Drugs , 编辑部邮箱 ,2009年10期
- 【分类号】R914
- 【被引频次】9
- 【下载频次】684