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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 investigate the synthetic process of cefpiramide, the third generation cephalosporin antibiotic. Methods: (2R) -2 - [(4-hydroxy-6-methyl-3-pyridyl) carboxamido] -2- (4 -hydroxyphenyl) acetic acid which is then coupled to the side chain (6R, 7R) -3 - [(-methyl- 1 H-tetrazol-5-yl) thio] -7 -amino-8-oxo-5-thia -1-azabicyclo [4,2,0] oct-2-ene-2-carboxylic acid (7-ACA-MMT) was used to synthesize the final product cefpiramide. Results: The total yield of the reaction was 19.42%. The compound was confirmed by 1H-NMR and IR spectra to be cefpiramide. Conclusion: The determination of cefpiramide synthesis process enhances the yield and improves the efficiency.