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麻保沙星的合成工艺研究
引用本文:严智,郑国钧. 麻保沙星的合成工艺研究[J]. 化学试剂, 2007, 29(11): 701-703
作者姓名:严智  郑国钧
作者单位:北京化工大学,生命科学与技术学院,北京,100029
摘    要:介绍了一种麻保沙星的绿色合成工艺。以2,3,4,5-四氟苯甲酸为原料,经酰氯化后与3-(N-甲基-甲酰肼基)-丙烯酸乙酯偶联、环合,与4-甲基哌嗪缩合、水解、环合,氨水中和得到目标产物,总收率为47.7%。与传统工艺相比,该法原料易得,实验步骤少,收率高,操作简单,具有一定的工业化前景。

关 键 词:麻保沙星  喹诺酮  合成
文章编号:0258-3283(2007)11-0701-03
修稿时间:2007-05-11

Study on new process for synthesizing marbofloxacin
YAN Zhi,ZHENG Guo-jun. Study on new process for synthesizing marbofloxacin[J]. Chemical Reagents, 2007, 29(11): 701-703
Authors:YAN Zhi  ZHENG Guo-jun
Affiliation:College of Life Science and Technology,Beijing University of Chemical Technology,Beijing 100029,China
Abstract:A green process for preparing marbofloxacin was described.The target compound was prepared starting from 2,3,4,5-tetrafluorobenzoic acid,via acyl chlorination,coupling with 3-(N-formylmethylhydrazono)-propionic acid ethyl ester,cyclization,condensation with N-methylpiperazine,hydrolysis by KOH solution,cyclization by formic acid and formaldehyde,and neutralization with aqueous ammonia,with the total product yield reaching 47.7%.Compared to the conventional method,this process has many advantages,including cheap starting material,simple procedure,short reaction time,which showed good perspective for commercial application.
Keywords:marbofloxacin  quinolone  synthesis
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