奎宁类化合物研究进展

Research Progress in Quinine Compounds

本文介绍了奎宁类化合物的发展历史,并分析了奎宁的化学结构。奎宁类化合物不仅可以作为催化剂,有效催化Michael/Mannich反应、Aza-Henry反应、环加成反应和不对称烯烃异构化反应,并且还可作为其他配体,已经成为不对称合成领域中的不可或缺成员。化学家为了寻找更有效的催化剂及配体,以奎宁类生物碱为前体,对其结构进行改造,改造位点主要集中在C-9位羟基、C-6'位甲氧基、奎宁双环的氮原子和环外烯键上,制备了众多催化剂及配体。此外,奎宁类化合物具有多种独特的生物效应,主要表现在抗疟原虫活性和杀虫活性研究方面。以奎宁为杀虫剂先导结构的优化与杀虫构效关系的系统研究将促进新农药创制学科的发展。

This paper introduces the development history of quinine compounds,and analyses the chemical structure of quinine. Quinine compounds,as catalysts and ligands,can effectively catalyze the reaction of Michael/Mannich,Aza-Henry,cycloaddition and asymmetric olefin isomerization,and can be used as other ligands,playing an important role in asymmetric synthesis. Firstly,in order to discover more effective catalysts and ligand,chemists have been working to modify the structure of such compounds with quinine alkaloids as precursors. The modification sites are mainly concentrated at the C-9 hydroxyl,C-6＇ methoxyl,nitrogen atoms of dual ring and an out-ring doublebond,and many catalysts and ligands were prepared on this basis. Secondly,quinines have a variety of unique biological effects,mainly in the study of antimalarial activity and insecticidal activity. The systematic research on structure optimizations and quantitative structure-activity relationship（ QSAR） of quinine derivatives as insecticidal agents will promote development of new pesticide innovation.