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门冬氨酸芦氟沙星的合成
引用本文:景士云,柳丽新,牟春福. 门冬氨酸芦氟沙星的合成[J]. 沈阳药科大学学报, 2008, 25(7): 553-555
作者姓名:景士云  柳丽新  牟春福
作者单位:哈药集团制药总厂,黑龙江哈尔滨,150046
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。

关 键 词:门冬氨酸芦氟沙星  喹诺酮  药物合成
收稿时间:2007-12-10

Synthesis of rufloxacin aspartate
JING Shi-yun,LIU Li-xin,MU Chun-fu. Synthesis of rufloxacin aspartate[J]. Journal of Shenyang Pharmaceutical University, 2008, 25(7): 553-555
Authors:JING Shi-yun  LIU Li-xin  MU Chun-fu
Affiliation:(The General Pharmaceutical Factory of Harbin Pharmaceutical Group ,Harbin 150046,China)
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][1,4]benzothiazine-6-carboxylic acid via four steps. The target compound was prepared by means of chelation, substitution, hydrolysis and salt formation reaction. Result The total yield was 62.7%. Conclusion The synthetic method is suitable for industrial production.
Keywords:rufloxacin aspartate  quinolone  synthesis
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