巴洛沙星的合成工艺改进

Process Improvement on the Synthesis of Balofloxacin

对巴洛沙星(Balofloxacin)合成工艺进行改进。以1-环丙基-6,7-二氟-8-甲氧基-4-氧代-1,4-二氢喹啉-3-羧酸乙酯为起始原料,经保护、缩合、水解等反应制得抗菌药巴洛沙星。总收率为58.9%。本工艺反应条件平和,成本较低,收率较原工艺有所提高。

To synthesize balofloxacin and to improve the synthetic procedure,Balofloxacin,an antibiotic,was synthesized through protection,reduction and hydrolysis from 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-oxo-3-quinoline carboxylic acid ethyl ester,and a total yield of 58.9% was achieved.This improved procedure is applicable to old industrial process.