【摘要】 目的合成喹诺酮类抗菌药门冬氨酸芦氟沙星。方法以9,10-二氟-7-氧-2,3-二氢-7H-吡啶并[1,2,3-de][1,4]苯并噻嗪-6-羧酸为起始原料,经螯合、取代、水解、成盐4步反应制得门冬氨酸芦氟沙星。结果制得门冬氨酸芦氟沙星,总收率为62.7%。结论该工艺适合工业化生产,为芦氟沙星的制剂研究提供了一个新的原料药。更多还原

【Abstract】 Objective To synthesize rufloxacin aspartate,a new quinolone antibacterial drugs,by a new method.Methods Rufloxacin aspartate was synthesized from 9,10-difluoro-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de]benzothiazine-6-carboxylic acid via four steps.The target compound was prepared by means of chelation,substitution,hydrolysis and salt formation reaction.Results The total yield was 62.7%.Conclusions The synthetic method is suitable for industrial production.A new raw medicine was provided with the research of rufloxacin preparation.更多还原