大理大学学报 ›› 2023, Vol. 8 ›› Issue (8): 25-29.

• 药学 • 上一篇    下一篇

Depresteroside选择性酯基水解条件优化

赖玉霞,郭海慧,秦子康,单 方,王福生*   

  1. (大理大学药学院,云南大理 671000)

  • 收稿日期:2023-02-20 修回日期:2023-03-01 出版日期:2023-08-15 发布日期:2023-07-11
  • 通讯作者: 王福生,教授,博士,E-mail:wfsyn@163.com。
  • 作者简介:赖玉霞,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(82260679);云南省地方本科高校基础研究联合专项资金项目(2019FH001-002)

Optimization of Selective Ester Hydrolysis Conditions for Depresteroside

Lai Yuxia, Guo Haihui, Qin Zikang, Shan Fang, Wang Fusheng*   

  1. (College of Pharmacy, Dali University, Dali, Yunnan 671000, China)

  • Received:2023-02-20 Revised:2023-03-01 Online:2023-08-15 Published:2023-07-11

摘要: 目的:为从Depresteroside(1)中高效获得化合物Secologanolyl-7-loganate(2)、马钱苷酸(3)和Demethylsecologanol(4),对其水解条件进行考察和优化。方法:采用单因素法考察碱种类及用量、反应温度、反应时间和碱浓度等因素对1的水解产物2、3和4收率的影响。结果:当用3.3当量0.10 mol/L Na2CO3溶液,45 ℃下加热反应12 h,仅生成化合物2,收率达87.2%;当用7.6当量0.10 mol/L NaOH溶液,45 ℃下加热反应13 h,可完全生成化合物3和4,收率分别为89.0%和90.8%。结论:优化的水解条件能明显提高2、3和4的收率。

关键词: font-family:Times New Roman, ">Depresterosidefont-family:Times New Roman, ">;水解反应;font-family:Times New Roman, ">Secologanolyl-7-loganatefont-family:Times New Roman, ">;马钱苷酸;font-family:Times New Roman, ">Demethylsecologanol

Abstract: Objective: To efficiently obtain the compounds Secologanolyl-7-loganate(2), Loganinic acid(3) and Demethyl-secologanol(4) from Depresteroside(1), the hydrolysis conditions were investigated and optimized. Methods: The effects of alkali type and dosage, reaction temperature, reaction time and alkali concentration on the yield of hydrolyzed products 2, 3 and 4 of 1 were investigated by single factor method. Results: When 3.3 equivalent 0.10 mol/L Na2CO3 solution was heated at 45 ℃ for 12 hours, only compound 2 was produced, and the yield reached 87.2%. Compounds 3 and 4 can be completely synthesized by using 7.6 equivalent 0.10 mol/L NaOH solution at 45 ℃ for 13 hours with yields of 89.0% and 90.8%, respectively. Conclusion: The optimized hydrolysis conditions can obviously improve the yield of 2, 3 and 4.

Key words: font-family:Times New Roman, ">Depresterosidefont-family:Times New Roman, ">;font-family:Times New Roman, "> hydrolysis reactionfont-family:Times New Roman, ">;font-family:Times New Roman, "> Secologanolyl-7-loganatefont-family:Times New Roman, ">;font-family:Times New Roman, "> Loganic acidfont-family:Times New Roman, ">;font-family:Times New Roman, "> ">Demethylsecologanol

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