摘    要 从事药物化学研究的研究者在药物开发的过程中都需要合成大量的化合物，研究他们的生物药理活性和结构也是极为重要的，通过大量的研究表明，绝大多数具有生物活性的化合物是杂环有机化合物，它们在医学、农业领域都十分重要，并且很多含有苯基哌嗪基团、喹啉基团、噁二唑基团的杂环化合物都有很高的生物活性。它们具有消炎、杀菌、抗癌、止痛、抗疟疾等医药功效，在医学和农业领域有着广泛的应用，许多类似的杂环化合物在临床上已经被用作消炎、抗癌、杀菌的药物。因此，通过人工合成这些具有生物活性的杂环化合物，是目前化学在医药和农药方面的研究热点。鉴于此，我们将采用药物设计的拼合原理，人工的将这些具有生物活性的基团拼合在同一个化合物中，由于物质的结构决定物质性质，我们希望通过物质结构的叠加来使化合物的生物活性叠加，合成结构新颖且具有多重生物活性的衍生物，并且能够提高药物的生物活性。90246

   本论文分为以下两部分：

   第一部分为文献综述部分：

   文中对喹啉衍生物的合成方法、生理活性、药理活性做了较全面的阐述，并且对苯基哌嗪、苯并咪唑、噁二唑的合成和性质做了简要的介绍。

   第二部分为实验部分，可分为三步：

（1）2-哌嗪醛-3-喹啉醛的制备，2-（2-哌嗪喹啉-2-基）苯并咪唑的合成 

（2）确定反应（1）和（2）的反应条件，并合成一定量各步产物，2-氯甲基-5-苯基,-1,3,4-恶二唑的合成 

（3）目标化合物合成条件及分离纯化条件的确定并合成目标化合物 

Researchers engaged in medicinal chemistry research in the process of drug development requires a large number of compounds, study their biological pharmacological activity and structure is of great importance, through a large number of studies have shown that the vast majority of the bioactive compounds are organic heterocyclic compounds, they are very important in the field of medicine, agriculture, and many contain phenylpiperazine groups, quinoline, oxadiazoles reactive heterocyclic compounds have very high biological activity。They have the anti-inflammatory, antiseptic, anti-cancer, pain, such as malaria medicine effect, has been widely used in medicine and agriculture fields, many of these heterocyclic compounds in clinic has been used as anti-inflammatory, anticancer, bactericidal drugs。Therefore, by synthesising these heterocyclic compound with biological activity, and is the chemical research focus in the field of medicine and pesticide。In view of this, we will use the split principle of drug design, these bioactive artificial groups split in the same compound, due to the structure determine physical properties of material, we hope that by superposition of the structure of the material to make the superposition of the bioactive compounds synthesis of novel structure and has multiple biological activity of derivatives, and can improve the biological activity of drugs。

This thesis is pided into the following two parts:

The first part is the literature review part:

This paper the synthesis of quinoline derivatives, biological activities and pharmacological activities made a more comprehensive description of and phenyl piperazine, benzene and imidazole, oxadiazoles the synthesis and properties of a brief introduction。源Q于W优E尔A论S文R网wwW.yOueRw.com 原文+QQ75201,8766

The second part is the experiment part, can be pided into three steps:

(1) - 3-2 - piperazine aldehyde quinoline the preparation of aldehydes, 2 - (2 - piperazine quinoline - 2 - base) benzene and the synthesis of imidazole

(2) to determine the reaction (1) and (2) the reaction conditions, and the synthesis of a certain amount of each step, 2 - methyl chloride - 5 - phenyl, 1 and 4 - oxadiazoles synthesis