Secologanol酰化产物的合成及其反应条件研究

Study on the Synthesis and Reaction Conditions of Secologanol Acylation Products

目的:为了改进裂环烯醚萜苷类成分Secologanol的抗阿尔茨海默病活性,拟对Secologanol进行结构修饰,合成其相应酰化产物,以期增强其衍生物的结构稳定性及活性,为进一步结构修饰打下基础。方法:通过控制酰化剂的当量及反应时间,将Secologanol分别与乙酸酐、苯甲酰氯进行酰化反应。结果:可快速、高效地得到相应的乙酰化产物和苯甲酰化产物。结论:合成了新的Secologanol酰化产物1、3、4和5。反应的重现性好,产率高,酰化产物结构稳定,可用于进一步的结构修饰和活性测试。

Objective:To improve the anti-Alzheimer′s disease activities of secoiridoid glycoside Secologanol.The aim of this study is to modify the structure of Secologanol and synthesize its corresponding acylation products,so as to enhance the structural stability and activity of its derivatives and lay a foundation for further structural modification.Methods:Secologanol was acylated with acetic anhydride and benzoyl chloride respectively by controlling the equivalent of acylating agent and its reaction time.Results:The acetylation and benzoylation products could be synthesized quickly and efficiently.Conclusion:New Secologanol acylation products 1,3,4 and 5 are synthesized.Besides,the reaction has good reproducibility with high yield and stable structure of acylation products,which can be used for further structural modification and activity test.