Abstract

The efficient total syntheses of four biologically interesting natural glucosides Ethylconiferin, Butylconiferin, 2’-Butoxyethylconiferin and Balajaponin B, have been achieved for the first time starting from commercially available Vanilline via concise reaction sequence of 8–10 steps with the overall yield of 26–41%. This work definitely laid the foundation for the further pharmacological study of this kind of natural compounds. Meanwhile, currently developed approach could be used as a general synthetic strategy for the syntheses of other monolignol glucosides and their derivatives, and provides an opportunity for further study of the structure-activity relationship of this kind of glucosides.

摘要

从市售的香兰素开始，通过8-10个步骤的简捷反应序列，总产率为26-，首次成功地获得了四种生物学上有趣的天然葡萄糖苷乙基松柏油，丁基松柏油，2'-丁氧基乙基松柏油和Balajaponin B的有效总合成。 41％。这项工作无疑为进一步研究这种天然化合物奠定了基础。同时，目前开发的方法可以用作合成其他单木酚糖苷及其衍生物的一般合成策略，并为进一步研究这种糖苷的构效关系提供了机会。