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萜类化合物——柳珊瑚烯酸是新类型的可逆性乙酰胆碱酯酶抑制剂。对小鼠、猫、狗的高度毒性也是一般萜类化合物所罕见的。本文报道了一系列衍生物的合成,发现柳珊瑚烯酸化学结构中:双键、羰基、羧基均对生物活性有巨大贡献,特别是前两者。由于该酸具有五个手性碳,故羧基还原为醇后,得两个差向异构体,400MHz’HNMR确定其构型。并对该酸及其酯进行量化计算,初步分析了生物活性与电荷密度间的关系。
Terpenoids - willowan acid is a new type of reversible acetylcholinesterase inhibitor. The high toxicity to mice, cats and dogs is also rare in common terpenoids. In this paper, we report the synthesis of a series of derivatives and find out that in the chemical structure of ligustilide, double bonds, carbonyl groups and carboxyl groups all contribute greatly to the biological activity, especially the former two. Since the acid has five chiral carbons, the carboxyl group is reduced to an alcohol to give two epimers, which are confirmed by 400 MHz’HNMR. The acid and its esters were quantified, and the relationship between biological activity and charge density was analyzed.