头孢匹胺的合成工艺研究

Studies on Synthetic Process of Cefpiramide

目的:探讨第3代头孢类抗菌药物——头孢匹胺的合成工艺。方法:以4-羟基-6-甲基-2-吡喃酮为原料合成(2R)-2-[(4-羟基-6-甲基-3-吡啶)甲酰胺基]-2-(4-羟基苯基)乙酸,再与侧链(6R,7R)-3-[(-甲基-1H-四唑-5-基)硫基]-7-氨基-8氧代-5-硫杂-1-氮杂双环[4,2,0]辛-2-烯-2-羧酸(7-ACA-MMT)反应合成得最终产品头孢匹胺。结果:反应总收率为19.42%,化合物经过核共振氢谱(1H-NMR)、红外图谱(IR)确证结构为头孢匹胺。结论:头孢匹胺的合成工艺确定增强了产率,提高了效率。

Objective：To study the synthetic process of cefpiramide in the 3 rd generation cephalosporin antibiotic drugs.Methods：Using 4-hydroxyl-6-methyl-2-pyrone as raw materials,（2R）-2-[4（-hydroxyl-6-methyl-3-pyridine）carboxamide]-2-（4-hydroxyl phenyl）acetic acid was produced,then condensation was conducted with（6 R,7 R）-3-[（methyl-1H-tetrazole-5）sulfenyl]-7-amino-8-oxo-5-thio-1-azabicyclo-[4,2,0]-2-octylene-2-carboxylic acid,and cefpiramide was synthesized.Results：The total yield of reactants was 19.42%,and structure of product was characterized by 1H-NMR,and IR.Conclusion：The synthesis process 1 of cefpiramide described here has advantages of high yield and efficiency.