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氟喹诺酮药物中间体合成研究进展
引用本文:徐兆瑜.氟喹诺酮药物中间体合成研究进展[J].化工科技市场,2009,32(1):35-39.
作者姓名:徐兆瑜
作者单位:安徽省化工研究院,安徽,合肥,230041
摘    要:介绍了合成喹诺酮药物-些重要中间体所取得的新进展,这些中间体包括:2,3,4-三氟~4-硝基苯、2,4-二氯-5-氟苯甲酸、4-丁酰氯、2,6-二氯-5-氟烟酰乙酸乙酯、2,4-二氯-5-氟苯乙酮、2,4-二氯氟苯等。另外,对某些合成方法的改进作了较详细叙述,如:2,4-二氯氟苯、2,4-二氯-5-氟苯甲酸等。如其中以1,2,3-三氯苯为起始原料,经硝化、氟化两步反应制得的1,2,3-三氟-硝基苯产品质量分数大于99%,收率达60%。

关 键 词:医药中间体  喹诺酮  抗菌素

Progress in synthesis of intermediates for quinolone antibacterial agents
Xu Zhaoyu.Progress in synthesis of intermediates for quinolone antibacterial agents[J].Chemical Technology Market,2009,32(1):35-39.
Authors:Xu Zhaoyu
Institution:Xu Zhaoyu ( Anhui Research Institute of Chemical Industry,Hefei 230041, China )
Abstract:New advance of some important intermediates for synthsizing quinolone antibacterial was introduced. These intermediates include 2, 3, 4 - trifluoronitrobenzene - g - nitrobenzene, 2, 4 - dichlor - 5 - fluorobenzoic acid, 4 - n - butyryl chloride,2,4 - dichlor - 5 - fluorobenzonic acid and ethyl - 2,6 - dichlor - 5 - fluoro nicotinoy acetate, and 2 ,d - dichlor fluorbenzene etc.. In addition, expounded improvement of some synthetic methods, such as 2,4 - dichlor fluor- benzene ,2,4 - dichlor - 5 - fluorobenzoic acid, etc. , if taking 1,2,3 - trifluoro - 4 - nitrobenzene sythesized by two processes of nitration and fluorinatin with 1,2,3 - trichlorobenzene as raw material. Content and of product was over 99%, and yield was 60%.
Keywords:medicine  intermediates  fluroquinolone  antibacterial agents
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