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巴洛沙星的生产新工艺
A NEW IMPROVED TECHNOLOGY FOR PRODUCTION OF BALOFLOXACIN
【摘要】 结合生产中的实际情况,对现有合成路线进行了优化设计,探索出了适合工业化生产的巴洛沙星的新工艺。用螯合法把化合物1-环丙基-6,7-二氟-1,4二氢-8-甲氧基-4-氧代-3-喹啉羧酸乙酯(DFQ-Et)螯合制得硼螯合物(1-环丙基-6,7-二氟-1,4二氢-8-甲氧基-4-氧代-3-喹啉羧硼二乙酯)[DFQ-B(OAc)2],再与3-甲氨基哌啶缩合,水解得到巴洛沙星,总收率75.2%。并对巴洛沙星进行了结构表征,该工艺反应条件温和,原料易得,操作简便,产率高,成本较低,适合工业化生产。
【Abstract】 A novel route for the synthesis of balofloxacin from DFQ-B(OAc)2 and 3-methylaminopipe- ridine was studied.The structure of the product identified was by IR,NMR.The total yield was 75.2%.Compared with the literature process,the improved method has the advantages of mild condi- tions,simple operation,easy isolation,high yield,safe and environmental benignity.
【基金】 国家自然科学基金项目(20473026)。
- 【文献出处】 精细石油化工 ,Speciality Petrochemicals , 编辑部邮箱 ,2008年01期
- 【分类号】TQ463.53
- 【被引频次】4
- 【下载频次】227