| 麻保沙星的合成工艺研究 |
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| 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 |
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| 作者姓名： | 严智 郑国钧 |
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| 作者单位： | 北京化工大学,生命科学与技术学院,北京,100029 |
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| 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。
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| 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 |
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| YAN Zhi,ZHENG Guo-jun. Study on new process for synthesizing marbofloxacin[J]. Chemical Reagents, 2007, 29(11): 701-703 |
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| Authors: | YAN Zhi ZHENG Guo-jun |
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| Affiliation: | College of Life Science and Technology,Beijing University of Chemical Technology,Beijing 100029,China |
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| 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. |
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| Keywords: | marbofloxacin quinolone synthesis |
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