门冬氨酸芦氟沙星的合成  

Synthesis of rufloxacin aspartate

作　　者：景士云[1] 柳丽新[1] 牟春福[1] 

机构地区：[1]哈药集团制药总厂,黑龙江哈尔滨150046

出　　处：《沈阳药科大学学报》2008年第7期553-555,共3页Journal of Shenyang Pharmaceutical University

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。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] [1, 4] 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.

关 键 词：门冬氨酸芦氟沙星 喹诺酮 药物合成 

分 类 号：R914.5[医药卫生—药物化学]