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。
A novel route for the synthesis of balofloxacin from DFQ-B（OAc）2 and 3-methylaminopiperidine 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 conditions, simple operation, easy isolation, high yield, safe and environmental benignity.
出处
《精细石油化工》
CAS
CSCD
北大核心
2008年第1期56-59,共4页
Speciality Petrochemicals
基金
国家自然科学基金项目(20473026)。
关键词
巴洛沙星
螯合法
抗菌剂
balofloxacin
production technology
identification
