本文選題：亞甲基吲哚酮 + N-甲氧基苯甲酰胺�。� 參考：《東北師范大學(xué)》2017年碩士論文

【摘要】：含氮化合物因良好的生物活性和藥物活性而被廣泛應(yīng)用于醫(yī)藥、農(nóng)藥、化工等相關(guān)領(lǐng)域。C-N鍵的構(gòu)建是合成含氮化合物的有效方法之一,而C-H鍵的直接官能團(tuán)化反應(yīng),尤其是sp~2C-H鍵的直接胺化反應(yīng)無需底物的預(yù)活化,可直接將胺基經(jīng)濟(jì)高效的引入到指定位點(diǎn)而受到廣泛的關(guān)注。近年來,芳烴C-H鍵的胺化反應(yīng)已取得較好的研究成果。然而關(guān)于烯烴C-H鍵的胺化反應(yīng)的報(bào)道相對(duì)較少,傳統(tǒng)的烯烴胺化反應(yīng)需要外加氧化劑、過渡金屬催化劑和配體等,通常存在著金屬催化劑價(jià)格昂貴、有毒、殘留等問題,限制了其在有機(jī)合成、制藥工業(yè)等領(lǐng)域的進(jìn)一步應(yīng)用。因此發(fā)展一種無金屬催化、氧化還原中性、條件溫和的烯基C-H的胺化反應(yīng)很有意義。本論文以亞甲基吲哚酮為底物,N-甲氧基苯甲酰胺為氮源,四甲基胍為催化劑,在100℃的條件下,實(shí)現(xiàn)了無金屬催化的烯基C-H鍵的酰胺化反應(yīng)。反應(yīng)過程中不需要外加氧化劑,也無需底物的預(yù)活化就能實(shí)現(xiàn)C-H鍵的直接官能化反應(yīng)。因此,我們發(fā)展了一種無金屬參與的、條件溫和的,操作簡(jiǎn)單的烯基C-H鍵的胺化反應(yīng),該反應(yīng)為合成多取代的烯胺類化合物提供了一種有效的合成途徑。
[Abstract]:Nitrogen-containing compounds are widely used in pharmaceutical, pesticide, chemical and other related fields because of their good biological activity and drug activity. The construction of C-N bond is one of the effective methods for the synthesis of nitrogen-containing compounds. In particular, the direct amination reaction of sph2C-H bond without substrate pre-activation can directly introduce the amine group to the designated site economically and efficiently, so it has attracted wide attention. In recent years, the amination reaction of aromatic C-H bond has achieved good results. However, there are relatively few reports on the amination of C-H bonds of olefins. Traditional olefin amination reactions require the addition of oxidants, transition metal catalysts and ligands, etc. It limits its further application in organic synthesis, pharmaceutical industry and other fields. Therefore, it is significant to develop a metal-free, redox neutral, mild amination reaction of alkenyl C-H. In this paper, N-methoxy benzoamide was used as nitrogen source and tetramethylguanidine as catalyst. The amidation of alkenyl C-H bond without metal was realized at 100 鈩，

本文編號(hào)：2110735