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摘要在医药工业中，喹啉及其衍生物都是合成药物的重要中间体，近年来，人类不断的开发出了许多含喹啉环的新型药物。喹啉及其衍生物具有抗肿瘤、抗疟疾、抗菌等药理活性，对人类新药研究具有一定的科学意义。在有机药物合成中，N-苯基哌嗪也是一类非常重要的药物中间体。苯基哌嗪及其衍生物具有抗癌、抗菌、抗结核、抗头痛等重要的药理活性。它是许多具有生物活性化合物的重要组成部分。46810
根据大量文献报道，[2+2]环加成、1,3-偶极环加成反应分别是构建四元、五元杂环的经典方法。所以我们的主要工作是将N-苯基哌嗪作为取代基引入到喹啉杂环分子中，并通过1，3-偶极环加成反应合成一系列具有潜在生物活性且结构新颖的喹啉衍生物，合成出了一系列含有N-苯基哌嗪的喹啉类衍生物。期望获得有潜在生物活性的化合物，为药物的筛选提供合成方法和先导化合物。
本论文分为以下两个部分：
第一部分为文献综述部分：
该部分对喹啉、N-苯基哌嗪的重要合成方法以及生理、药理活性等的研究状况作了比较系统的综述；同时还就1，3-偶极环加成反应等对含喹啉衍生物及N-苯基哌嗪的衍生物进行结构修饰的环合反应作了简要介绍。
第二部分为实验部分，主要工作如下：
1、 新型N-苯基哌嗪喹啉衍生物1-(4-芳基-2-噻唑基)-3-芳基-5-[2-(4-苯基哌嗪-1-基)喹啉-3-基]-吡唑啉的合成与表征；
2、 对产物结构进行元素分析、MS、1HNMR确认，并对其波谱性质进行了分析和讨论。
In the pharmaceutical industry, quinoline and its derivatives are important intermediates for the synthesis of drugs. In recent years, human beings continue to develop many new quinoline ring-containing drugs. Quinoline and its derivatives have anti-tumor, anti-malarial, anti-bacterial and other pharmacological activity, with certain scientific significance for human drug research. In an organic Drug Synthesis, N- phenyl-piperazine is also a very important class of drug intermediates. Phenyl piperazine and its derivatives have anti-cancer, anti-bacterial, anti-tuberculosis, anti-headaches and other important pharmacological activity.
It is an important component of many biologically active compounds. According to many reports, [2 + 2] and 1,3-dipolar cycloaddition reactions are the classic method used for synthesizing the five-membered, four-membered heterocycles respectively. So our main job is to N- phenyl-piperazine as a substituent is introduced into the quinoline heterocyclic molecules, and by 1,3-dipolar cycloaddition reactions synthesize a series of novel quinoline with potential biological activity and structure derivatives, synthesized a series of quinoline derivatives containing N- phenylpiperazine. We expect to obtain compounds with potential biological activity, provide synthetic methods and lead compounds for drug screening.
This thesis is pided into two parts:
The first part of the literature review section:
This part of the quinoline, N- phenylpiperazine synthesis methods as well as physiological and pharmacological activity of the situation in the study were relatively systematic exposition; It also briefly describes the 1,3-dipolar cycloaddition reactions on quinoline derivatives and N- phenyl-piperazine derivatives structural modification of derivatives cyclization.
The second part is the experimental section, the main work is as follows:
1,Synthesis and Characterization of Novel N- phenyl-piperazine derivatives of quinolone 1- (4-aryl-2-thiazolyl) -3-carbonyl-5- [2- (4-phenyl-piperazin-1-yl) quinoline-3-yl] - pyrazoline.
2,The product structure of elemental analysis, MS, 1HNMR confirmed and the analysis and discussion of its spectral properties.
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