| 氟喹诺酮类抗菌剂卡德沙星的合成研究 |
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| 引用本文： | 仲琰,吴斌. 氟喹诺酮类抗菌剂卡德沙星的合成研究[J]. 中国药学杂志, 2008, 43(13): 1028-1030 |
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| 作者姓名： | 仲琰 吴斌 |
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| 作者单位： | 1.东南大学化学化工学院 南京 210096;2.南京医科大学药学院 南京 210029 |
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| 摘 要： | 目的研究氟喹诺酮类抗菌剂卡德沙星的合成工艺。方法以3-二氟甲氧基-2,4,5-三氟笨甲酸为起始原料,经酰氯化、缩合、脱羧、醚化、环丙胺置换、环合、螯合、上甲基哌嗪、水解得本品。结果卡德沙星经红外、核磁、质谱确证。结论本法原料易得,操作简单,总收率高,而且整个过程不需柱色谱纯化,是理想的工业化生产路线。
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| 关 键 词： | 卡德沙星 氟喹诺酮类抗菌剂 合成 |
| 收稿时间： | 2007-07-15; |
Studies on Synthesis of Fluoroquinolone Antimicrobial Agent Caderofloxacin |
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| ZHONG Yan,WU Bin. Studies on Synthesis of Fluoroquinolone Antimicrobial Agent Caderofloxacin[J]. Chinese Pharmaceutical Journal, 2008, 43(13): 1028-1030 |
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| Authors: | ZHONG Yan WU Bin |
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| Affiliation: | 1．School of Chemistry and Chemical Engineering，Southeast University，Nanjing 210096，China；2．School of Pharmacy，Nanjing Medical University，Nanjing 210029，China |
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| Abstract: | OBJECTIVE To synthesize caderofloxacin,a fluoroquinolone antimicrobial agent.METHODS Caderofloxacin was prepared from 3-difluoromethoxy-2,4,5-trifluorobenzoic acid by acylating reaction,followed by condensation,decarboxylation, etherification,replacement of cyclopropyl,cyclization,chelation,piperazination,hydrolysis,successively.RESULTS The structures of intermediates and caderofloxacin were identified by IR,1H-NMR and MS.CONCLUSION The method avoided using column chromatograph in all steps and it is convenient for industry production. |
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| Keywords: | caderofloxacin fluoroquinolone antimicrobial agent synthesis |
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