摘要
采用硼鳌合物法,以1-环丙基-6,7-二氟-8-甲氧基-4-氧代-1,4-二氢-3-喹啉羧酸乙酯和(S,S)-2,8-二氮杂双环[4.3.0]壬烷为原料合成莫西沙星,对影响收率的主要因素进行了考察,合成鳌合物的最佳工艺条件为:反应温度90℃,反应时间3h,收率>90%;合成莫西沙星的最佳条件:乙腈作溶剂、三乙胺作缚酸剂,鳌合物与(S,S)-2,8-二氮杂双环[4.3.0]壬烷的物质的量的比为1:1.1,反应时间为3h,产物收率80.5%。该方法反应条件温和,操作和后处理相对简单,收率较高。
By means of the borate chelate, moxifloxacin is prepared by 1-cyclopropyl-6,7-difluoro-8-methoxyl-4-oxo-1,4-dihydro- quinoline-3-carboxylic acid ethyl ester and (S,S)-2,8-diazabicyclo[4.3.0]nonane. Factors on the synthesis are studied, and the optimum reaction conditions are obtained: reaction time is 90℃, reaction time is 3h, yield of the product is over 90%. Best conditions for the synthesis of moxifloxacin is: ratio of triethylamine as the acid acceptor, chelate compound and (S,S)-2,8-diazabicyclo[4.3.0]nonane is 1:1:1, reaction time is 3 h, yield of the product is 80.5%. Reaction conditions are mild, after-treatment of the operation is relatively simple and the yield is higher.
出处
《化工生产与技术》
CAS
2007年第6期15-17,41,共4页
Chemical Production and Technology
基金
山西省教委资助项目(96025)
关键词
莫西沙星
亲核取代
硼整合物
合戍
moxifloxacin
mucleophilic substitution
borate chelatet
synthesis
