高效合成三取代中氮茚化合物

发布时间：2018-04-16 19:42

本文选题：杂环化合物 + 中氮茚　；参考：《华东理工大学》2017年硕士论文

【摘要】：本论文主要由四部分组成。第一章是杂环化合物的介绍和应用、中氮茚的介绍和合成方法概述以及α溴代烯醛参与的反应简介。第二章包含了两部分。第一部分是以α-溴代烯醛和2-取代的吡啶衍生物为起始原料在碳酸铯的作用下实现了三取代中氮茚结构化合物的合成。通过该方法不仅可以以较高的产率合成吡咯并吡啶类化合物,还可以以中等的产率合成结构类型更多样的吡咯并[1,2-a]喹啉化合物和咪唑并[1,2-a]吡啶类化合物。该方法具有无需过渡金属、无需氧化剂、无需催化剂、起始原料简单、操作简便、反应迅速以及官能团兼容性良好等优点。第二部分发展了一种利用2-(吡啶-2-基)-乙酸乙酯与(E)-查耳酮在空气作为氧化剂的条件下通过铜催化的[3+2]环合反应"一锅法"合成中氮茚骨架化合物的方法。本方法具有着氧化剂以及催化剂廉价易得、对环境友好等优势。第三章是利用发展出的高效合成中氮茚骨架化合物及其衍生物的方法并且同时结合本课题组之前的研究成果,我们设计并合成了一系列改造后的化合物来进行抗宫颈癌生物活性测试。第四章是全文总结,总结了本论文所叙述的工作,包括两种三取代中氮茚化合物的合成方法以及利用此方法合成具有潜在抗肿瘤活性的药化分子等。
[Abstract]:This thesis mainly consists of four parts. The first chapter is the introduction and application of heterocyclic compounds, indolizine introduction and overview and synthesis method of alpha bromo aldehyde in the reaction profile. The second chapter consists of two parts. The first part is to pyridine derivatives a-bromo-carboxylic aldehyde and 2- substituted as the starting material in cesium carbonate under the action of the three synthesis of substituted indolizine compounds. This method can yield higher to the synthesis of pyrrole and pyridine compound can also yield with the synthesis of a variety of types of secondary structure of pyrrolo [1,2-a] quinoline compounds and imidazo [1,2-a] pyridine compounds. This method has without transition metal, without oxidant without catalyst, simple starting materials, simple operation, quick response and functional compatibility is good. The second part is developed by using a 2- (-2- pyridine base) - Ethyl acetate (E) and chalcone in air as through [3+2] cyclization reaction "copper catalyzed one pot synthesis of indolizine skeleton compounds under oxidant conditions. This method has an oxidation agent and catalyst is cheap, environmentally friendly and other advantages. The third chapter is the use of azaindene method skeleton compound and its derivatives in the development of efficient synthesis and combined with the results from previous studies of our research group, we designed a series of compounds and modified to anti cervical cancer bioassay was synthesized. The fourth chapter is the summary, summarized in this thesis, two methods of synthesis of three substituted indolizine compounds and the use of this method for the synthesis of potential anti-tumor active drug molecules.

【学位授予单位】：华东理工大学
【学位级别】：硕士
【学位授予年份】：2017
【分类号】：O626;TQ460.1

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