阿维巴坦关键中间体合成工艺研究+NMR谱图
毕业论文关键词： 阿文巴坦；β-内酰胺类；广谱；哌啶酮
The study on synthesis the key intermediate of Avibactam
Abstract： Avibactam (formerly NXL104, AVE1330A) is a synthetic non-β-lactam substances, within the β-lactamase inhibitor of Ambler A, class C and partially Ambler D grade enzymes active. Although not β-lactamase chemical structure, similar to part of Avibactam cephem bicyclic ring system, and Avibactam has been shown to the bonded covalently bound to β-lactamases. Avibactam potential roles include the suspected or to prove by resistant Gram-negative bacilli produce extended-spectrum β-lactamase (ESBL), Klebsiella pneumoniae carbapenemase (KPC) and / or produced within AmpC β-lactamase treatment. According to the literature we use sulfur ylide generation of reactive intermediates to produce the desired imine third step, a sulfur ylide substituted with chlorine, and then in an acid off under boc protection ring closure under basic conditions, the use of propyleneyl sodium borohydride reduction we need to choose the configuration, use oxalic acid salt formation, recrystallization, to obtain high purity product. We design two synthetic routes to synthesis the key intermediate piperidone, one is a 5-hydroxy-2-carboxy pyridine, and the other one is L-glutamic acid diethyl ester hydrochloride as starting materials, paying attention to controlling two lines'reaction temperature and reaction time at the same time, making the process of synthesis intermediate of piperidone more simple, less environmental pollution, easy industrialization and optimize the two routes in a way to the maximum extent.
KeyWords：Avibactam; β-lactamse; extended spectrum ; piperidone
目 录
1 绪论 1
1.1 课题背景与意义 1
1.2 阿文巴坦的简介 1
1.2.1 阿文巴坦的相关化学信息 2
1.2.2 阿文巴坦的应用价值 3
1.2.3 阿文巴坦的制备合成方法 3
1.3 本课题主要研究内容 4
1.3.1 阿文巴坦关键中间体合成路线的研究现状 4
1.3.2 阿文巴坦合成反应路线优化 6
2 实验部分 8
2.1 实验试剂和仪器 8
2.1.1 实验试剂 8
2.1.2 实验仪器 9
2.1.3 试剂的物理常数 10
2.2 主要反应原理 11
2.2.1 线路一 11
2.2.2 线路二 14
2.3 实验步骤 15
2.3.1 路线一 15
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