左氧氟沙星绿色合成工艺  

Green Synthesis of Levofloxacin

作　　者：杨朱红[1,2] 杨秋燕 李亚美 吴戈亮 韩德全 秦宝福[1] 

机构地区：[1]西北农林科技大学生命科学学院,陕西杨凌712100 [2]河南天方药业股份公司,河南驻马店463000

出　　处：《浙江化工》2013年第9期13-15,22,共4页Zhejiang Chemical Industry

摘　　要：介绍一种合成左氧氟沙星的新工艺。以(2,3,4,5)-四氟苯甲酰氯为起始原料,与3-乙氧基丙烯酸乙酯反应,然后L-氨基丙醇进行胺化反应,环合、水解后与N-甲基哌嗪缩合制得左氧氟沙星,总收率为50.15%。该工艺操作简单,环境污染小,符合绿色化学发展方向,值得进一步研究和推广。New process for preparing Levofloxacin was described. The target was prepared from （2,3,4,5 ）- fluorobenzoic chloride, which reacted with ethyl 3-ethoxyacrylate, amination with S-（＋ ）-2-aminopropanol, cyclization ,hydrolysis and condensation with N-methyl piperazine. The total yield was 50.15%. The process has many advantages, such as simple operation, less environmental pollution. In line with the green chemistry development direction, it deserves further research and popularization.

关 键 词：左氧氟沙星 3-乙氧基丙烯酸乙酯 绿色合成 

分 类 号：TQ463[化学工程—制药化工] R944[医药卫生—药剂学]