摘要
目的合成盐酸莫西沙星。方法以1-环丙基-6,7-二氟-1,4-二氢-8-甲氧基-4-氧代-3-喹啉羧酸乙酯为起始原料,经硼螯合反应、与(S,S)-2,8-二氮杂双环〔4.3.0〕壬烷缩合、酸化并加水结晶制备得盐酸莫西沙星。结果合成的盐酸莫西沙星总收率约为75%。结论:本合成工艺对硼螯合反应进行了优化,不使用腐蚀和毒性的氯化锌,能够达到很好的螯合效果;螯合物与壬烷的缩合产物通过简便的后处理方式,即直接酸化继而加水析晶,制备得盐酸莫西沙星,总收率在75%左右。产品纯度高,单个杂质小于0.1%,总杂质小于0.2%,适合工业化生产。
Objective synthesize moxifloxacin hydrochloride. Method：take the 1-cyclopropyl-6, 7-difluoro-1, 4-dihydro-8-methoxy- 4-oxo- 3-ethyl quinoline carboxylate as the original materials and after the borate chelate reaction, condensation with the （S, S）-2,8-diazabicyclo[4.3.0] nonane, acidification and crystallization by adding water, we can prepare the moxifloxacin hydrochloride. The results show that the total recovery of the synthetic moxifloxacin hydrochloride is about 75%. Conclusion shows that the synthetic process takes optimization of the borate chelate reaction, and without the use of corrosive and virulent zinc chloride, a good chelation effect can be achieved, For the condensed products produced by the chelate and nonane, through simple post-processing method, can directly have the acidification reaction and then have the crystallization reaction by adding water, finally get the preparation of moxifloxacin hydrochloride, which has the total recovery of about 75%. This product has a high purity besides, the impurity of each one is less than 0.1% and the total impurity is less than 0.2%, which is suitable for industrial production.
出处
《当代化工研究》
2016年第10期121-122,共2页
Modern Chemical Research
关键词
盐酸莫西沙星
螯合
缩合
工艺优化
moxifloxacinhydrochloride
chelation
condensation
processimprovement
