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]壬烷亲核取代反应、酸化制备盐酸莫西沙星.结果合成的盐酸莫西沙星总收率为70%.结论本合成路线对硼螯合反应进行了优化,不使用强腐蚀性、有毒的氯化锌,无需高温回流,可以达到很好的螯合效果;亲核取代反应选用无机碱碳酸钾作缚酸剂,加入相转移催化剂溴化正丁基铵,缩短了反应时间,提高了收率.该工艺操作简单,生产成本低,减少了环境污染,适合工业化生产.
Objective To synthesize moxicloxacin hydrochloride. Methods Moxicloxacin hydrochloride was synthesized from 1 - cyelopropyl - 6,7 - difluoro - 1,4 - dihydro - 8 - methoxyl - 4 - oxoquinoline - 3 - diethyl carboxylate via boric coordination, nucleophilic substitution with （ S, S） - 2,8 .- diazabicyclo [ 4.3.0 ] nonane and acidification. Results The total yield of moxieloxaein hydroehloride was 70%. Conclusion The boric coordination was optimized in this synthesis process to avoid using of corrosive and toxic reagent zinc chloride and reflux at high temperature. The reaction time of nucleophilic substitution was shorten and the yield was improved by using inorganic base potassium carbonate as acid binding agent and tetra - n - butyl ammonium bromide （ TBAB ） as phase transfer catalyst. This process was more suitable for industrial production with simple operation, low production cost and low environment pollution.
出处
《齐鲁药事》
2011年第12期683-684,共2页
qilu pharmaceutical affairs
关键词
盐酸莫西沙星
硼螯合反应
亲核取代
相转移催化剂
Moxifloxacin Hydrochloride
Boric coordination
Nucleophilic substitution
Phase transfer catalyst
