左氧氟沙星合成工艺改进研究

Technogical Improvement for Synthesis of Levofloxacin

对左氧氟沙星的工艺进行了优化,以(2,3,4,5)-四氟苯甲酰氯为起始原料,经酰化,胺化,环合制得左氧氟环合酯,然后用无水哌嗪与左氧氟环合酯缩合,经硫酸二甲酯甲基化后水解精制得左氧氟沙星。与原工艺相比,用无水哌嗪代替N-甲基哌嗪,提高了产品的收率和质量,降低了成本,减少了环境污染,技术指标符合CP2010左氧氟沙星要求。

The levofloxacin process was optimized. Levofloxacin was prepared with 2,3,4,5 -Tetrafluorobenzoyl chloride as the starting material, by acylation, amination, and cyclization left oxyfiuoride cyclization ester was obtained, and then Piperazine and left oxyfluoride cyclization ester condensation, after methylation by dimethyl sulfate, hydrolysis, condesation. Comparing to the old process, Piperazine instead of N - methylpiperazine, process was improved with many advantages, such as improving the yield and quality of the product, reducing the cost, reducing environmental pollution, and technical indicators in line with the CP2010 Levofloxacin requirements.