具有重要生物活性的啤酒花多酚类天然产物的全合成和结构修饰研究

项目名称： 具有重要生物活性的啤酒花多酚类天然产物的全合成和结构修饰研究

项目编号： No.21202028

项目类型： 青年科学基金项目

立项/批准年度： 2013

项目学科： 有机化学

项目作者： 李惠静

作者单位： 哈尔滨工业大学

项目金额： 25万元

中文摘要： 啤酒花多酚类天然产物如原花色素、异黄腐酚、黄腐酚和8-异戊二烯基柚皮素是人类未来的 "健康卫士"和"抗癌之星"，其独特的药食同源性特征和潜在的应用前景使其成为目前国际社会的关注热点。本项目在前期工作的基础上，分析啤酒花多酚类天然产物的结构特征，发掘其各个关键片断单元的结构要求，拟开展含有原花色素信息的黄腐酚等类化合物的合成研究，A型原花色素类天然产物的全合成研究，以及含有黄腐酚等信息的A型和B型原花色素类化合物的合成研究。在项目实施过程中，结合反合成分析理念和项目组报道的协同反应理念，根据目标分子的结构进行巧妙设计，力争在国际上率先完成一系列具有重要生物活性的A型原花色素类天然产物的全合成，为加快后续的构效关系研究和结构优化打下基础。

中文关键词： 多酚类天然产物；合成；啤酒花；苯并吡喃；生物活性的

英文摘要： Hops polyphenol natural products, such as proanthocyanidins, isoxanthohumol, xanthohumol and 8-prenylnaringenin, are regarded as potential "health guardian" and "anticancer star". These natural polyphenols have attracted increasing attention thanks to their unique medicine food homology properties and their great potential applications.Accordingly, the total synthesis and structure modification of these natural products becomes a high priority in the field of chemistry, biology and medicine sciences. In connection with our ongoing work in this field, herein we plan to achieve the synthesis of xanthohumol analogues based on the struture of proanthocyanidins, the total synthesis of A-type proanthocyanidins, as well as A-type and B-type proanthocyanidin analogues based on the struture of xanthohumol. Based on the concepts of "retrosynthesis" as well as "synergistic model" developed by us before, we would try our best to accomplish several first asymmetric total syntheses of bioactive A-type proanthocyanidin natrural products via desired synthetic routes explored by studying their unique chemical structures.The total synthesis would in turn facilitate the corresponding structure-activity relationship studies and structure optimization. To achieve this goal, we will develop new synthetic routes, study some reaction m

英文关键词： polyphenols；synthesis；hops；chromenes；bioactive