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摘要:近年来，随着抗生素的大量使用甚至是滥用，细菌的耐药性问题日益严重。噁唑烷酮类抗菌药是继磺胺类和喹诺酮类后的一类新型化学全合成抗菌药，具有抑制多重耐药革兰阳性菌的作用。噁唑烷酮具有独特的作用机制，使得该类药物与其他蛋白质合成抑制剂的抗菌药物没有交叉耐药性，备受国内外医药界关注。
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开发具有新化学结构、抗菌机制独特、抗耐药性强新型噁唑烷酮类抗菌药是我们本次实验的主要目的。我们将选择一条最佳合成路线，以得到新型噁唑烷酮化合物合成工艺中的重要的中间体。实验时以对苯二胺为原料先与二碳酸二叔丁基酯反应保护一个胺基，再与氯甲酸苄酯结合，最后与(S)-N-[2-乙酰氧基-3-氯丙基]乙酰胺进行成环反应得到目标产物。6350
本研究关键中间体和最终目标产物的结构经1H-NMR确认。关键词：噁唑烷酮；苯胺衍生物；重要中间体
The synthesis of aniline derivative substituted by oxazolidinone ring
Abstract:In recent years, with extensive use of antibiotics and even abuse, the growing resistance of bacterial has becoming a serious problem. Oxazolidinone antibacterial agents is a new class of chemical total synthetic of antibacterial drugs following sulfonamides and quinolones, which can inhibit multi-drug-resistant Gram-positive bacteria. Oxazolidinone having a unique mechanism, This unique mechanism of oxazolidinone antibacterial drugs makes these drugs have no cross-resistance with other antimicrobial agents which also Inhibit the synthesis of protein ,it has attracted attention from the medical profession at home and abroad.Developing a new oxazolidinone antimicrobial drug with new chemical structure,unique mechanism of antibacterial and anti-resistance strength is the main purpose of our experiment.This topic is just the preliminary work of the project, we will select an optimal synthetic route to synthesis an important intermediate in the new oxazolidinone compound process.We use phenylenediamine as the starting material to react with Di-tert-butyl dicarbonate to protecting an amine,then combined with benzyl chloroformate,finally,react with (S)-N-[2-acetoxy-3- chloro-propyl] ,then the final product was obtained.
The final product and its intermediates has been confirmed by 1H-NMR.
Keywords：oxazolidinone; aniline derivative; important intermediate
目 录
1 绪论 1
1.1 抗菌药概述 1
1.2 噁唑烷酮类药物 1
1.3 利奈唑胺 3
1.3.1 利奈唑胺概述 3
1.3.2 利奈唑胺的作用机制 4
1.4 课题研究目的 4
2 文献综述及方法论证 6
2.1 利奈唑胺的结构改造 6
2.1.1 A环的改造 6
2.1.2 B环的改造 6
2.1.3 C5侧链的改造 7
2.1.4 C环的改造 7
2.2 利奈唑胺合成方法 8
2.2.1 以R构型的环氧氯丙烷为原料合成利奈唑胺 8
2.2.2 以S-缩水甘油醛为原料合成利奈唑胺 9
2.2.3 以R-缩甘油丁酸酯为原料合成利奈唑胺 10