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 Rg₃ was 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.

吉林市科技局项目（201222316）