刺桐碱类化合物的不对称合成及生理活性研究

刺桐生物碱具有的复杂结构和多样的生物活性一直受到科学家的注目，其多环结构为合成化学家利用于研究成环形反应的新方法。.本课题组发展了4-氨基酚的酰胺衍生物氧化去芳构化策略合成刺桐、吲哚和六氢吡咯并[2,3-b]吲哚环系的方法，而氧化去芳构化之后1,4 -加成反应不仅产生第一不对称中心，而且去对称化后可以产生连续不对称中心，对于高效构建多环系统是至关重要的。本项目将设计合成一系列催化剂应用于刺桐生物碱分子内二烯酮Michael不对称加成反应，并将其应用于几个刺桐生物碱类似物的不对称合成，并首次对二聚体erythrivarines A和B进行合成研究，同时设计合成一系列刺桐生物碱类似物并进行初步生理活性研究。

The erythrina alkaloids have attracted interest because of their interesting structures and their range of useful biological activities. Erythrina alkaloids have characteristic polycyclic structures, and they have proved to be popular target molecules for synthetic chemists to exploit new methods for ring-forming reactions..Recently we reported a process towards the synthesis of highly functional erythrina alkaloid, oxindole and hexahydropyrrolo[2,3-b]indole ring systems through an oxidative dearomatization strategy from amide derivatives of 4-aminophenoln,and the dearomatization is followed by a 1,4-addition to produce the first asymmetric center. The formation of the stereocenter is crucial because it determines whether or not the synthesis, will be enantioselective, and the desymmetrization of these systems mediated by an asymmetric catalyst is therefore very important. In this project, an enantioselective intramolecular Michael reaction will to be studied for the formation of erythrina alkaloids from.cyclohexadienones using designed catalyst. A series of erythrina alkaloid analogues were to be designed and synthesized，their biological activity will to be studied.