摘    要

随着杂环化学的不断发展，人们发现杂环化合物有着比单体更好的生物活性和药物活性。如何研发出药效更好的新型治疗疾病药物已经是当今热门研究之一，大量的研究表明三唑类衍生物、喹啉类化合物、噻二唑类衍生物合成的药物都普遍具有良好的生物活性以及杀菌谱广泛，药物的效果好，内部吸收性好等优点。杂环类喹啉和喹啉衍生物在医药、工业等领域应用广泛，根据药物药效的加和原理，把不同药效的杂环结构组合在同一个分子内，可以预期得到药效更好、具有药物广谱性的杂环化合物。85420

我们的研究工作首先是将 1,2,4-三唑作为取代基引入到喹啉环的2位，得到关键中间体2-三唑基喹啉-3-甲醛，再利用喹啉3位活泼的醛基合成了新型的2,3-二杂环取代的喹啉衍生物。

本论文分为以下两部分： 第一部分为引言：主要介绍了喹啉、三氮唑等杂环化合物及其研究的进展状况，包括这些药物的药理活性、合成方法等。

第二部分为实验部分：

本部分主要介绍了以合成出的2-氯--3-喹啉甲醛为原料，经过多步反应合成出含有喹啉、三唑、噻二唑等含有喹啉母环的新型杂环化合物。首先我们把2号位喹啉上的醛直接氧化成脂，在把脂肼解，然后继续反应得到重要的中间产物氨基巯基，最后合成出噻二唑的产物3-（2-（1H-1,2,4-三唑-1基)-喹啉-3-基）-6-对苯取代-[1,2,4]三唑并[3,4-b][1,3,4]噻二唑，并用波谱学方法对目标化合物的结构进行了确证。

毕业论文关键词：杂环化合物；喹啉； 1,2,4-三氮唑； 噻二唑

Abstract In recent years, with the continuous development of heterocyclic chemistry, it has been found that heterocyclic compounds have better bioactivity and drug activity than monomers。 How to develop new drugs for better treatment of diseases has been one of the hottest research, which has a large number of studies show that three triazole derivatives; quinolines; drug Thiadiazolen two azole derivatives synthesis generally have good bioactivity and wide bactericidal spectrum, drug effects, advantages of internal absorptive capacity and so on。 In addition to these heterocyclic compounds in medicine can synthesize the excellent new drugs, on the research of 1,2,4- triazole heterocyclic derivatives of fungicidal activity, three triazole compounds have good biological activity in the world wide attention, and is the largest pesticide company developed a series of new three triazole fungicides。 A lot of quinoline and quinoline derivatives can also be used as dyes in textile dyeing auxiliaries and hair dyes。 While Thiadiazolen two azole derivatives is because itself is five membered heterocyclic compounds containing N, S atoms, with significant aromatic and conjugated effect, is now very important in the field of chemical intermediates, in agriculture, industry and medicine industry has a very important application。 In the aspect of pesticide, the two triazole derivatives can be developed into a new type of pesticide with good bactericidal property and low toxicity。 In industry, the two triazole derivatives have close and stable structure, good bearing capacity and lubricity。 These advantages make the synthesis of heterocyclic compounds more and more attention by experts in pesticide and medicine。

The main subject of our study is to introduce 1,2,4-triazole and phenylpiperazine as substituents into 2 position of the quinoline molecule, obtained the key intermediates 2-(1,2,4-triazole-1-yl)-6-methyl-3-quinilinecarboxaldehyde and 2-(4-phenylpiperazin-1-yl)-quinolin-3-carbaldehyde, and exploited the carbaldehyde group of 3 position, three series of novel and 38 potentially biologically active 2,3-disubstituted quinoline derivatives were synthesized。 The structures of the obtained target compounds were elucidated by MS, IR, 1H NMR, and elemental analyses。