基于氧化偶联反应构建喹唑啉（酮）衍生物的研究
发布时间：2018-11-14 16:17
【摘要】：含氮杂环化合物在医药和农药方面都具有广泛的应用前景,特别是广泛存在于自然界中的喹唑啉和喹唑啉酮类化合物,其在生物活性和药理活性方面都有显著价值,因此关于它们合成方法的研究一直以来都是化学家们关注的焦点。目前,传统合成喹唑啉酮的方法依然存在一些缺陷,例如:初始原料制备繁琐;反应条件比较苛刻;反应需要特殊后续处理以及底物适应性差;所以,研究一种高效、便捷合成喹唑啉酮类化合物的方法成为了一大挑战;另外,对喹唑啉化合物的4号位进行官能团化也是近几年研究领域的一大热点,。本论文主要研究了利用我们实验室合成的几种喹唑啉-N-氧化物和醇类、甲酰胺类化合物在温和的条件下发生氧化偶联反应得到喹唑啉酮类化合物及喹唑啉-N-氧化物类衍生物。本论文主要包括以下三部分研究内容:(1)本论文介绍了在CuCO_3·Cu(OH)_2催化下,喹唑啉-N-氧化物和醇类在60℃下便可合成一系列喹唑啉酮类化合物,反应条件温和,操作简单,底物适用范围广。(2)本论文介绍了铜催化喹唑啉-N-氧化物和甲酰胺类化合物合成新型的喹唑啉酮氨基甲酸酯类化合物的反应,该化合物不仅有喹唑啉酮的结构,也有氨基甲酸酯的结构,这两个结构在生物活性和药理方面都有很好的应用前景。(3)本论文介绍了在KI催化下,喹唑啉-N-氧化物和烷基醇类在100℃下发生氧化偶联反应,实现了Csp2-Csp3的构建,该反应条件绿色环保,且操作简单。本论文实现了在温和的条件下高效绿色的合成喹唑啉酮类化合物及喹唑啉-N-氧化物类衍生物,反应操作简单,原料廉价易得。
[Abstract]:Nitrogen-containing heterocyclic compounds are widely used in medicine and pesticides, especially quinazoline and quinazolinone compounds, which are widely found in nature. Therefore, the study of their synthesis methods has been the focus of chemists. At present, there are still some defects in the traditional method of synthesis of quinazolinone, such as: the initial raw material preparation is cumbersome, the reaction conditions are harsh, the reaction needs special follow-up treatment and the substrate adaptability is poor; Therefore, the study of an efficient and convenient method for the synthesis of quinazolinones has become a major challenge. In addition, the functionalization of quinazoline compounds at position 4 is a hot topic in recent years. In this paper, several quinazoline-N-oxides and alcohols synthesized in our laboratory were studied. Quinazolinone derivatives and quinazoline-N-oxide derivatives were obtained by oxidative coupling reaction of formamide compounds under mild conditions. The main contents of this thesis are as follows: (1) in this thesis, a series of quinazolinones can be synthesized at 60 鈩，
本文编号：2331671
[Abstract]:Nitrogen-containing heterocyclic compounds are widely used in medicine and pesticides, especially quinazoline and quinazolinone compounds, which are widely found in nature. Therefore, the study of their synthesis methods has been the focus of chemists. At present, there are still some defects in the traditional method of synthesis of quinazolinone, such as: the initial raw material preparation is cumbersome, the reaction conditions are harsh, the reaction needs special follow-up treatment and the substrate adaptability is poor; Therefore, the study of an efficient and convenient method for the synthesis of quinazolinones has become a major challenge. In addition, the functionalization of quinazoline compounds at position 4 is a hot topic in recent years. In this paper, several quinazoline-N-oxides and alcohols synthesized in our laboratory were studied. Quinazolinone derivatives and quinazoline-N-oxide derivatives were obtained by oxidative coupling reaction of formamide compounds under mild conditions. The main contents of this thesis are as follows: (1) in this thesis, a series of quinazolinones can be synthesized at 60 鈩，
本文编号：2331671
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