一种合成二氢黄酮醇衍生物的简易方法,优先出版.pdfVIP

有机化学DOI:10.6023/cjoc201605044 研究简报 Chinese Journal of Organic Chemistry NOTE 一种合成二氢黄酮醇衍生物的简易方法 周宗宝 王红 陶凯奇 叶晓川 胡春玲* (湖北中医药大学中药化学与中药资源省级重点实验室，湖北，武汉 430065) 摘要 以2-羟基查尔酮衍生物为原料，在低温条件下，以THF 为溶剂，在H O /(C H ) NH 体系中， 2 2 2 5 2 高收率地实现一系列二氢黄酮醇类衍生物的合成. 考查了反应温度、反应溶剂、碱添加剂的种类和比例以 及氧化剂的种类和比例对该反应的影响，确定了最优反应条件。此合成方法具有操作简单、条件温和及后 处理方便等特点. 此外，所合成产物的结构经核磁共振谱表征确证. 关键词 2-羟基查尔酮衍生物；二氢黄酮醇类衍生物；简易的方法 A Facile Method to Prepare Dihydroflavonol Derivatives Zhou, Zong-bao Wang, Hong Tao, Kai-qi Ye, Xiao-chuan Hu, Chun-ling* (Key Laboratory of Chinese Medicine Chemistry and Chinese Herbal Compound of Hubei Province, Hubei University of Traditional Chinese Medicine, Wuhan 430065, China) Abstract A series of dihydroflavonol derivatives were synthesized by the reaction of 2- hydroxyl chalcone derivatives with H O / (CH CH ) NH system in anhydrous THF under low temperature. The influences of reac- 2 2 3 2 2 tion temperature, reaction solvents, the kinds and proportion of alkaline additive and oxidants on this reaction were investigated, and the optimal reaction conditions were determined. This method has the advantages o f simple op- eration, mild conditions and convenient post-treatment. Besides, all synthetic products were fully characterized by NMR spectra. Keywords 2 - hydroxyl chalcone derivatives; dihydroflavonol derivatives; facile method 二氢黄酮类化合物为黄酮类C-2,3 位的双键氢化后的衍生物，此类化合物在植物中多数带有羟基或甲氧基，当 C-3 位上带有羟基时，通称为二氢黄酮醇类(dihydroflavonols). 某些二氢黄酮醇类化合物表现出极佳的生物活性，如 花旗松素((taxifolin)