头孢匹罗的合成

Synthesis of cefpirome

丙炔胺和环戊酮在无水乙醇中回流反应5 h生成2,3-环戊烯并吡啶,收率55%。7-氨基头孢烷酸和2-甲氧亚氨基-2-(2-氨基-4-噻唑基)-(z)-硫代乙酸苯胼噻唑酯(AE活性酯)发生酰化反应生成头孢噻肟酸,收率90%。在三甲基碘硅烷作用下,头孢噻肟酸与2,3-环戊烯并吡啶反应,生成头孢匹罗,收率65%1。H NMR对产物及中间体进行了鉴定。

2,3-Cyclopentenopyridine was prepared by reaction of cyclopentanone and propargylamine in absolute ethanol, refluxing 5 h, the yield was 55%. Cefotaxime acid was synthesized by 7-ACA and AE active ester, the yield was 90%. Then, in the presence of trimethyliodosiliane, cefpirome was obtained through the reaction of cefotaxime acid and 2,3-cyclopentenopyridine, the yield was 65 %. The structure of target substance and intermediate were determined by ^1H NMR.