| 甲磺酸帕珠沙星的合成 |
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| 引用本文： | 钱方,黎文海.甲磺酸帕珠沙星的合成[J].山西化工,2011,31(3):7-9,34. |
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| 作者姓名： | 钱方 黎文海 |
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| 作者单位： | 1. 南京医科大学附属南京市第一医院药剂科,江苏 南京,210006
2. 中国药科大学,江苏 南京,210017 |
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| 摘 要： | 研究了甲磺酸帕珠沙星的合成路线及工艺。以左旋氧氟沙星的中间体（S）-9，10-二氟-3-甲基-2，3-二氢-7-氧代-7H-吡啶1，2，3-de]1，4]苯并噁嗪-6-羧酸乙酯为起始原料，经亲核取代反应、酯水解并选择性脱羧、环合、水解、Hofmann降解、成盐，制得甲磺酸帕珠沙星，总收率49．4％。其化学结构经元素分析、^1H NMR、^13C NMR、MS得以确证。该合成路线及工艺适合工业化大生产。
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| 关 键 词： | 甲磺酸帕珠沙星 抗菌药 合成 |
Synthesis of pazufloxacin mesilate |
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| QIAN Fang,LI Wen-hai.Synthesis of pazufloxacin mesilate[J].Shanxi Chemical Industry,2011,31(3):7-9,34. |
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| Authors: | QIAN Fang LI Wen-hai |
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| Affiliation: | 1. Department of pharmacy, Nanjing First Hospital Affiliated to Nanjing Medical University, Nanjing Jiangsu 210006, China; 2. China Pharmaceutical University, Nanjing Jiangsu 210017, China) |
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| Abstract: | The synthetic route and improved process for the preparation of pazufloxacin mesilate were studied. Compound was synthesized from （S） -9,10-ditluoro-3-methyl-2,3-dihydro-7-oxo-7-H-pyrido 1, 2,3-de ] 1,4 ] benzoxazine-6-carboxylate by nucleophilic substitution, hydrolysis and selective decarboxylation, cyclic addition, hydrolysis. Hofmann degradation and salt formation, its overall yield was 49.4%. The chemical structure was confirmed by elemental analysis, IR, ^1H NMR, ^13C NMR, MS. This synthetic routy was suitable for industrial production. |
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| Keywords: | pazufloxacin mesilate antibacterial agent synthesis |
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