阿莫西林合成工艺改进

Improved synthetic technology of amoxicillin

目的阿莫西林合成工艺的改进。方法以6-APA为起始原料,工艺路线为6-APA胺盐溶液与混合酸酐反应得阿莫西林。结果目标产物的结构经元素分析、IR、~1H-NMR、^(13)C-NMR谱数据确证,且质量符合国家2005版药典。结论改进后的工艺新解决了原工艺酸酐反应不完全及水解等问题,操作简单、产品质量稳定、收率高、成本低、更适合工业化生产。

Objective To improve the synthetic technology of amoxicillin. Methods Amoxicillin was synthesized from a main raw material 6-aminopenicillanic acid（6-APA） and acid anhydrides by nucleophilic substitution. Results The structure of final product was confirmed by elemental analysis, IR, 1H-NMR, 13C-NMR and the qualities of final product measure up CP2005. Conclusion Compared with original process, the problems of the reaction of mixed acid anhydrides and hydrolyzation were solved. The improved process has high yield, low cost and is easy to operate, while the quality of products is much more stable and suitable for industrial production.