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

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。

Objective： To optimize the synthetic route of aspoxicillin, a semi-synthetic penicillin. Methods： Aspoxieillin 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.