舒巴坦酸制备工艺研究

Study on Preparation Process of Sulbactamic Acid

舒巴坦酸是人工合成的不可逆的竞争性β-内酰胺酶抑制剂,本身的抗菌活性弱,略强于克拉维酸,单用时仅对淋球菌和不动杆菌属有杀菌作用。但是,与青霉素类或头孢菌素类药物联用,能够出现明显的协同作用,并且极大地提高了青霉素类或头孢菌素类药物的抗菌活性,同时也扩大了抗菌谱,降低了耐药性。以6-APA为起始原料,经过重氮化、溴化、氧化及金属锌粉还原制得舒巴坦酸产品。该方法操作便捷,工艺稳定,收率高,产品质量好。

Sulbactam acid is an irreversible competitiveβ-lactamase inhibitor with weak antibacterial activity,slightly stronger than clavulanic acid,and only has bactericidal effect on gonococci and Acinetobacter spp.However,in combination with penicillin or cephalosporins,there can be obvious synergistic effects,which greatly improves the antibacterial activity of penicillins or cephalosporins,while also expands the antibacterial spectrum and reduces drug resistance.In this paper,sulbactam acid products were prepared via diazotization,bromination,oxidation and metal zinc powder reduction using 6-APA as the starting material.The method is convenient to operate,stable process,and has high yield and good product quality.