头孢尼西钠的合成工艺研究

Study on the synthesis of cefonicid sodium

为筛选头孢尼西钠合成的最佳工艺条件,采用7-氨基头孢烷酸(7-ACA)与5-巯基-1,2,3,4-四氮唑-1-甲基磺酸双钠盐(SMT)反应得到7-氨基-3-[[1-磺酸甲基-1-H-四唑-5-基)硫基]甲基]头孢霉烷酸(7-AMT)。7-AMT与D-(-)-甲酰基扁桃酰氯(FMC)反应,去除甲酰基保护基得头孢尼西酸。头孢尼西酸结晶成钠盐,得到合格产物头孢尼西钠。改进后的工艺路线缩短了生产周期,提高了产品的收率和质量,降低了生产成本。

In order to screen the optimal conditions for the synthesis of cefonicid sodium,7-aminocephalosporanic acid（ 7-ACA） and 5-mercapto-1,2,3,4-tetrazolium-Bis-sodium salt（ SMT） was reacted to give 7-amino-3-[[1-sulfonomethyl-1-H-tetrazol-5-yl） thio]methyl]cephem acid（ 7-AMT）. 7-AMT was reacted with D-（-）-formylmandelic acid chloride（ FMC） to remove cefonicid with formyl protection. Cephisinic acid crystallized into sodium salt to obtain qualified product cefonicid sodium. The improved process route shortens the production cycle,improves the product yield and quality,and reduces the production cost.