【摘要】：含氮雜環(huán)化合物在醫(yī)藥和農(nóng)藥方面都具有廣泛的應(yīng)用前景,特別是廣泛存在于自然界中的喹唑啉和喹唑啉酮類(lèi)化合物,其在生物活性和藥理活性方面都有顯著價(jià)值,因此關(guān)于它們合成方法的研究一直以來(lái)都是化學(xué)家們關(guān)注的焦點(diǎn)。目前,傳統(tǒng)合成喹唑啉酮的方法依然存在一些缺陷,例如:初始原料制備繁瑣;反應(yīng)條件比較苛刻;反應(yīng)需要特殊后續(xù)處理以及底物適應(yīng)性差;所以,研究一種高效、便捷合成喹唑啉酮類(lèi)化合物的方法成為了一大挑戰(zhàn);另外,對(duì)喹唑啉化合物的4號(hào)位進(jìn)行官能團(tuán)化也是近幾年研究領(lǐng)域的一大熱點(diǎn),。本論文主要研究了利用我們實(shí)驗(yàn)室合成的幾種喹唑啉-N-氧化物和醇類(lèi)、甲酰胺類(lèi)化合物在溫和的條件下發(fā)生氧化偶聯(lián)反應(yīng)得到喹唑啉酮類(lèi)化合物及喹唑啉-N-氧化物類(lèi)衍生物。本論文主要包括以下三部分研究?jī)?nèi)容:(1)本論文介紹了在CuCO_3·Cu(OH)_2催化下,喹唑啉-N-氧化物和醇類(lèi)在60℃下便可合成一系列喹唑啉酮類(lèi)化合物,反應(yīng)條件溫和,操作簡(jiǎn)單,底物適用范圍廣。(2)本論文介紹了銅催化喹唑啉-N-氧化物和甲酰胺類(lèi)化合物合成新型的喹唑啉酮氨基甲酸酯類(lèi)化合物的反應(yīng),該化合物不僅有喹唑啉酮的結(jié)構(gòu),也有氨基甲酸酯的結(jié)構(gòu),這兩個(gè)結(jié)構(gòu)在生物活性和藥理方面都有很好的應(yīng)用前景。(3)本論文介紹了在KI催化下,喹唑啉-N-氧化物和烷基醇類(lèi)在100℃下發(fā)生氧化偶聯(lián)反應(yīng),實(shí)現(xiàn)了Csp2-Csp3的構(gòu)建,該反應(yīng)條件綠色環(huán)保,且操作簡(jiǎn)單。本論文實(shí)現(xiàn)了在溫和的條件下高效綠色的合成喹唑啉酮類(lèi)化合物及喹唑啉-N-氧化物類(lèi)衍生物,反應(yīng)操作簡(jiǎn)單,原料廉價(jià)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，

本文編號(hào)：2331671