论文总字数：21125字

摘 要

含氮杂环化合物广泛存在于天然产物中，在医药、农业、工业以及基础研究等领域的应用受到科学界的广泛关注，研究此类化合物的合成方法具有重要的意义。近年来，大量有关噻唑烷酮类化合物的发展和生物活性的综述被报导。噻唑烷酮类化合物作为一种含氮杂环化合物 具有重要的意义，而且还表现出多种生物活性，如结核菌抑制，抗糖尿病，抗组胺和抗真菌活性。本文以苯胺、异硫氰酸苯酯和溴乙酰溴作为原料使用一锅法合成噻唑烷酮类化合物。

本文通过对反应体系溶剂、温度、时长三方面的筛选， 选定了最佳的反应条件：以DMF为溶剂，在60℃下加热回流6小时，顺利合成噻唑烷酮类化合物；选定了最佳反应条件之后，本文又通过目的产物的结构表征考察了此反应体系两个底物的普适性，得出结论此反应体系的两个底物普适性都很好。

本文开发了一种新的合成噻唑烷酮类化合物的方法，此方法使用的原料便宜易得、一锅法操作简单便捷、反应条件温和且耗能少，后处理方便，避免了有毒催化剂的使用，减少了噻唑烷酮类化合物的合成成本，提高了对环境的友好度，将会在 生化制药领域方面的研究发挥一定的价值。

关键词 氮杂环化合物 一锅法 噻唑烷酮

Abstract

Nitrogenous heterocyclic compounds are widely found in natural products. Their applications in medicine, agriculture, industry and basic research have attracted wide attention from scientists. It is of great significance to study the synthetic methods of such compounds. In recent years, a large number of reviews about the development and biological activities of thiazolidones have been reported. Thiazolone compounds are of great importance as a nitrogen-containing heterocyclic compound and also exhibit various biological activities such as tuberculosis inhibition, anti-diabetes, antihistamine and antifungal activity. In this paper, aniline, phenyl isothiocyanate and bromoacetyl bromide were used as raw materials to synthesize thiazolidinone compounds by one-pot method.

In this paper, the optimal reaction conditions were selected by screening the solvent, temperature and duration of the reaction system: DMF was used as solvent and heated at 60 ° C for 6 hours to synthesize thiazolidinone compounds. After the good reaction conditions, the generality of the two substrates of the reaction system was investigated by the structural characterization of the target product. It was concluded that the two substrates of the reaction system were universally applicable.

A new method for the synthesis of thiazolidinone compounds has been developed in this paper. The raw materials used in this method are cheap and easy to obtain, the one-pot method is simple and convenient to operate, the reaction conditions are mild and the energy consumption is low, the post-treatment is convenient, the use of toxic catalysts is avoided, the cost of synthesis of thiazolidinone compounds is reduced, and the environmental friendliness is improved. This method will be studied in the field of biochemical pharmaceuticals. Research and play a certain value.

Key Words：N-heterocycle compounds; One-Pot;Thiazolidinone derivatives;

目录

摘 要 II

Abstract III

第一章 文献综述 5

1.1 噻唑烷酮类化合物的概要 5

1.1.1噻唑烷酮类化合物的研究进展 5

1.1.2噻唑烷酮类化合物的基本结构 5

1.1.3噻唑烷酮类化合物的药理学研究 6

1.1.4噻唑烷酮类化合物的应用 6

1.2噻唑烷酮类化合物合成方法 7

1.2.1以硫脲为原料合成噻唑酮类化合物 7

1.2.2以巯基乙酸为原料合成噻唑烷酮类化合物 9

1.2.3其他合成噻唑烷酮类化合物的方法 10

1.3 课题研究的内容及意义 12

第二章 实验部分 13

2.1 仪器与试剂 13

2.1.1 仪器 13

2.1.2 试剂 13

2.2 最佳件筛选 14

2.2.1 实验操作 14

2.2.2 结果与分析 15

2.3 底物拓展 15

2.3.1 不同取代苯胺与各种异硫氰酸苯酯反应的实验流程 15

2.3.2不同取代苯胺与各种异硫氰酸苯酯反应的结果与分析 16

2.4 化合物的结构表征 18

第三章 总结 20

参考文献 21

致谢 23

第一章 文献综述

1.1 噻唑烷酮类化合物的概要

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