| 甲磺酸帕珠沙星的合成 |
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| 引用本文： | 智翠梅,温艳珍,王齐.甲磺酸帕珠沙星的合成[J].应用化工,2007,36(5):472-474. |
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| 作者姓名： | 智翠梅 温艳珍 王齐 |
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| 作者单位： | 太原科技大学,化学与生物工程学院,山西,太原,030021 |
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| 摘 要： | 研究氟喹诺酮类抗菌剂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-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、Hofrnann降解、成盐得甲磺酸帕珠沙星,总收率60.0%。其化学结构经元素分析,IR,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： | 氟喹诺酮类抗菌剂 甲磺酸帕珠沙星 合成 |
| 文章编号： | 1671-3206(2007)05-0472-03 |
| 修稿时间： | 2006-11-27 |
Synthesis of pazufloxacin mesilate |
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| ZHI Cui-mei,WEN Yan-zhen,WANG Qi.Synthesis of pazufloxacin mesilate[J].Applied chemical industry,2007,36(5):472-474. |
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| Authors: | ZHI Cui-mei WEN Yan-zhen WANG Qi |
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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-difluoro-3-methyl-7-oxo-2,3-dihydro-7H-pyrido 1,2,3-de]]benzoxazine-6-carboxylate by nucleophilic substitution,hydrolysis and selective decarboxylation,cyclic addition,hydrolysis.Hofmann degradation and salt formation,its overall yield was 60.0%.The chemical structure was confirmed by elemental analysis,IR,1H NMR,13C NMR,MS.This synthetic route is suitable for industrial manufacture. |
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| Keywords: | fluoroquinoione antibacterial agent pazufloxacin mesilate synthesis |
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