麻保沙星新合成路线研究

Research of New Process of Mabrofloxacin Synthesis

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.