离子液体辅助巴洛沙星的绿色合成  

Green Synthesis of Balofloxacin by Ionic Liquids

作　　者：何新蕾[1] 郝二军[2] 张玲[1] 邱盼盼[2] 

机构地区：[1]漯河医学高等专科学校,河南漯河462002 [2]河南师范大学化学化工学院

出　　处：《中国医学创新》2014年第24期127-129,共3页Medical Innovation of China

基　　金：河南省教育厅科学技术研究重点项目(13B350079)

摘　　要：目的:研究离子液体辅助巴洛沙星的合成路线。方法:以1-环丙基-6,7-二氟-1,4-二氢-8-甲氧基-4-氧代-3-喹啉硼二乙酯和3-甲胺基哌啶为起始原料,在绿色反应介质离子液体[bmim]PF6中合成新药巴洛沙星。结果:在离子液体中合成巴洛沙星,总产率为68.5%。最佳反应时间应控制在6 h左右;离子液体经过5次重复使用以后,新药巴洛沙星的收率才开始明显降低;在合成新药巴洛沙星时使用不同的离子液体对产品收率影响不大。结论:该方法反应条件温和,操作简便,产率高,产品纯度高,有机溶剂残留低等优点,且反应介质离子液体可循环利用。Objective：To study the synthesis of balofloxacin by ionic liquids.Method：Balofloxacin was synthesized from 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxoquinoline boron diethyl carboxy-late with 3-methylaminopiperidine in ionic liquids.Result：Balofloxacin was synthesized in ionic liquids,the total yield was 68.5%. The best response time should be controlled at about 6 h. Ionic liquid after repeated use for 5 times,the drug yield of Balofloxacin began to decrease. There was no effect for the product yield when used different ionic liquid to synthesize Balofloxacin.Conclusion：The method has the advantages of mild reaction condition,simple operation,high yield,high product purity,residual organic solvents is low,and the reaction medium ionic liquid can be recycled.

关 键 词：巴洛沙星 绿色合成 离子液体 

分 类 号：TQ463[化学工程—制药化工]