大理大学学报 ›› 2021, Vol. 6 ›› Issue (4): 10-13.

• 药学 • 上一篇    下一篇

Secologanol酰化产物的合成及其反应条件研究

王 乐,杨宗斌,王 甜,郭海慧,王福生   

  1. (大理大学药学院,云南大理 671000)
  • 收稿日期:2021-01-07 修回日期:2021-01-20 出版日期:2021-04-15 发布日期:2021-05-19
  • 通讯作者: 王福生,教授,博士,E-mail:wfsyn@163.com。
  • 作者简介:王乐,硕士研究生,主要从事天然药物化学研究。
  • 基金资助:
    国家自然科学基金项目(31360082;31860098);云南省地方本科高校(部分)基础研究联合专项资金项目
    (2019FH001-002)

Study on the Synthesis and Reaction Conditions of Secologanol Acylation Products

Wang Le, Yang Zongbin, Wang Tian, Guo Haihui, Wang Fusheng    

  1. (College of Pharmacy, Dali University, Dali, Yunnan 671000, China)
  • Received:2021-01-07 Revised:2021-01-20 Online:2021-04-15 Published:2021-05-19

摘要: [摘要]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。

关键词: [关键词]裂环烯醚萜苷, Secologanol, 结构修饰, 酰化产物

Abstract: 〔Abstract〕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.

Key words: 〔Key words〕seroiridoid glycoside, Secologanol, structural modification, acylation products

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