本文選題：鈀催化 + 烯烴　； 參考：《上海應(yīng)用技術(shù)大學》2017年碩士論文

【摘要】：雙胺化合物廣泛存在于生物活性體和天然產(chǎn)物中,同時,很多藥物分子中也含雙胺氮雜環(huán)結(jié)構(gòu)。因此,如何經(jīng)濟、環(huán)保、高效、快速地構(gòu)建C-N鍵,合成具有雙胺基團化合物越來越受到人們的關(guān)注。金屬催化烯烴進行雙官能團化,一步構(gòu)建雙胺化產(chǎn)物是目前最為簡便、直接、有效的方法。近年來,烯烴的雙胺化反應(yīng)有著很大的進展.,其中,使用高效的過渡金屬催化劑以及氮源,合成新型雙胺化合物無疑更具有研究價值和應(yīng)用前景。本文主要研究鈀催化烯烴的雙胺化反應(yīng),通過對溫度、溶劑、配體、催化劑等條件的篩選,發(fā)現(xiàn)當使用Pd(OAc)2為催化劑,2,2'-聯(lián)吡啶為配體,四氫呋喃為溶劑,以常見的、氧化性的N-氟代雙苯磺酰胺為氮源,在80 ℃下,空氣中即可高效得到雙胺化產(chǎn)物,最高可得90%的收率。此反應(yīng)可以廣泛地適用于各種不同取代基團的鄰烯基氮烷基苯甲酰胺底物,并且為含有異吲哚啉酮類骨架的藥物合成提供了有效的合成方法。同時,操作簡單、反應(yīng)條件溫和也使得該方法更具有廣闊的工業(yè)化前景。
[Abstract]:Diamine compounds are widely found in bioactive bodies and natural products. At the same time, many drug molecules also contain heterocyclic structures of diamine nitrogen.Therefore, more and more attention has been paid to the construction of C-N bonds and the synthesis of bisamine-containing compounds in an economical, environmentally friendly, efficient and rapid manner.Metal-catalyzed bifunctional alkenes and one-step construction of diamination products are the most convenient direct and effective methods at present.In recent years, great progress has been made in the diamination of olefins. Among them, the synthesis of new diamine compounds by using highly efficient transition metal catalysts and nitrogen sources undoubtedly has more research value and application prospect.The oxidized N-fluorobenzenesulfonamide was used as nitrogen source, and the highest yield of 90% was obtained from the diamination product in air at 80 鈩，

本文編號：1731902