β-内酰胺类抗生素氨曲南化学合成的研究进展

Advances in the Chemical Synthesis of Amitractam-lactam antibiotics

文章通过头孢他啶侧链活性酯和(3S-反式)-3-氨基-4-甲基-2-氧代-1-氮杂环丁烷磺酸为主要原料先合成叔丁酯氨曲南,然后在酸性条件下水解获得α-氨曲南,再通过无水乙醇条件下转晶获得β-氨曲南,并对合成产物进行表征。实验结果表明,合成产物为β-氨曲南,理化性质均能达到国家药品要求。

In this paper,tert-butyl aztreonam was synthesized from ceftazidime side chain active ester and(3 S-trans)-3-amino-4-methyl-2-oxo-1-aza-cyclobutane sulfonic acid as main raw materials,then hydrolyzed under acidic conditions to obtainα-aztreonam,and then transformed intoβ-aztreonam under anhydrous ethanol conditions,and the synthesized products were characterized.The experimental results show that the synthetic product isβ-aztreonam,and its physical and chemical properties can meet the national drug requirements.