舒巴坦氧化新工艺研究

Research on the New Oxidation Process of Sulbactam

研究了一种合成舒巴坦前体二溴代青霉烷砜酸的新工艺。该工艺以双氧水/三氟乙酸作为氧化体系,收率达到92%以上。随后用锌粉将二溴代青霉烷砜酸还原得到舒巴坦,总收率为74%(三步反应),质量满足药用标准。与传统的KMnO_(4)氧化法相比,该方法具有安全性高,后处理简单和环境友好的特点。

A new process for the synthesis of dibromopenicillanic sulfone acid,a precursor of sulbactam,was studied in this paper.In this process,H_(2)O_(2)/TFA was used as the oxidation system,and the yield was above 92%.A subsequent Zn powder reduction of dibromopenicillanic sulfone acid yielded sulbactam in 74%overall yield(three steps),and the quality met the standard of medicinal use.This method has the advantages of high safety,simple post-treatment and environmental friendliness compared with the traditional KMnO_(4)oxidation.