酒石酸催化转化原人参二醇组皂苷制备20(R)-人参皂苷Rg3

Catalytic conversion of protopanaxadiol saponins to 20(R)-ginsenoside Rg_3 by tartaric acid

目的选择性制备20(R)-人参皂苷Rg3,为其制备提供理论依据。方法以酒石酸为催化剂,原人参二醇(PPD)组皂苷为原料,通过单因素试验和正交试验对20(R)-人参皂苷Rg3的制备工艺进行优化,反应产物用HPLC进行定量分析。结果正交试验优化结果表明,PPD(10 mg/mL)和酒石酸(1.5 mol/L)于110℃反应2.5 h,人参皂苷Rb1、Rc、Rb2、Rb3和Rd基本全部转化,20(R)-人参皂苷Rg3的产率为50.15%,其非对映体过量百分比为93.12%。结论该方法操作简单,成本低廉,适宜工业化生产,对于推动20(R)-人参皂苷Rg3的药理活性研究具有重要意义。

Objective To prepare 20（R）-ginsenoside Rg3 selectively and to provide the theory basis for the preparation.Methods 20（R）-Ginsenoside Rg3 was prepared by hydrolyzing protopanaxadiol（PPD）-type saponins using tartaric acid as the catalyst.The preparation condition was optimized by one-factor experiment and orthogonal test,and the reaction products were analyzed by HPLC.Results The optimization result of orthogonal test showed that when PPD-type saponins（10 mg/mL） were hydrolyzed by tartaric acid（1.5 mol/L） at 110 ℃ for 2.5 h,all the ginsenosides Rb1,Rc,Rb2,Rb3,and Rd were converted,the yields of 20（R）-ginsenoside Rg3was 50.15%,and the diastereomer excess percentage（de%） was 93.12%.Conclusion This method is simple,low-cost,and suitable for the mass production,which is very important to promote the study on the pharmacological activities of 20（R）-ginsenoside Rg3.