Depresteroside选择性酯基水解条件优化

Optimization of Selective Ester Hydrolysis Conditions for Depresteroside

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。

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.