麻保沙星新合成路线研究  

Research of New Process of Mabrofloxacin Synthesis

作　　者：单国洋 姚礼高 蒋狄峰 丁路阳 侯仲轲 邱家军 Bruno Boisniere 

机构地区：[1]国邦医药化工集团有限公司,浙江绍兴312369

出　　处：《精细化工中间体》2015年第2期35-37,共3页Fine Chemical Intermediates

基　　金：国家科技部国际科技合作专项(2012DFA40940)

摘　　要：以2,3,4,5-四氟苯甲酰氯为起始原料,与3-(4-甲基哌嗪-1-基)-丙烯酸乙酯反应,再与N-甲基甲酰基肼环合缩哌、碱解,最后环合得到麻保沙星。方法工艺简单,收率高,质量好,大幅减少了废水废气排放,具有较高工业化价值。2,3,4,5-Tetrafluorobenzoyl chloride was used as the starting material to react with （E）-ethyl 3-（d- methylpiperazin-1-yl）acrylate. Then, this obtained intermediate reacted with N-methylformohydrazide to give a reaction mixture. In the end, this reaction mixture was hydrolized in akaline and a cyclization reaction was performed to give Mabrofloxacin. This novel method has the advantages of simple process, high yield, good quality, and little waste water emissions with high industrial value.

关 键 词：2 3 4 5-四氟苯甲酰氯 3-(4-甲基哌嗪-1-基)-丙烯酸乙酯 麻保沙星 

分 类 号：R931.74[医药卫生—生药学]