正交试验优化盐酸莫西沙星的合成工艺

摘要

Objective The technology of moxifloxacin hydrochloride was optimized by orthogonal test.Methods Orthogonal test was adopted to analyze the effect of reaction temperature,reaction time and crystallization time on the yield of moxifloxacin.Results The result showed that among the three factors,reaction temperature had the most significant effect while dosage of the reactants had the lest effect.The optimum reaction conditions were,reaction temperature,75～85℃; reaction time 2h; crystallization temperature 0～5 ℃.The yield of optimized process product was up 80％.Conclusion This method was warranted for the commercial process.%目的 盐酸莫西沙星的合成工艺优化.方法 以环丙基-7-{(S,S)-2,8-重氮-二环[4,3,0]壬烷-8-基}-6-氟-8-甲氧-1,4-二氢-4-氧代—3-喹啉羧酸-O3,O4-二乙酸根合硼合成盐酸莫西沙星.结果 通过正交试验考察反应温度,反应时间和结晶温度对盐酸莫西沙星的影响,结果表明3因素中,反应温度对盐酸莫西沙星的影响最大,结晶温度的影响最小,最佳反应温度为75～85℃,反应时间为2h,结晶温度为0～5℃.结论 在该条件下,盐酸莫西沙星成品收率稳定在80％以上,工艺简单可靠,成本低,适合工业化生产.