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响应面法优化 d,l-酒石酸催化 20(R)-人参皂苷 Rg3 的选择性制备。

Optimization of the selective preparation of 20(R)-ginsenoside Rg3 catalyzed by d, l-tartaric acid using response surface methodology.

机构信息

Department of Chemistry, Northeast Normal University, Changchun, China.

出版信息

Fitoterapia. 2013 Jan;84:213-21. doi: 10.1016/j.fitote.2012.11.011. Epub 2012 Dec 3.

Abstract

The optimization of the selective preparation of 20(R)-ginsenoside Rg3 converting protopanaxadiol type saponins (PPD saponins) by the commercially available d, l-tartaric acid was carried out using response surface methodology (RSM) based on a three-factor and six-level central composite design. The optimal 20(R)-ginsenoside Rg3 de% was predicted to be 94.52% in the combination of the factors (d, l-tartaric acid concentration 1.19mol/L, temperature 107.9°C and time 2.79h) through the canonical analysis with maximum responses. Under the optimum reaction conditions, the actual 20(R)-ginsenoside Rg3 de% was 96.49%. 20(R)-ginsenoside Rg3 (1) and 20(S)-ginsenoside Rg3 (2) were separated and identified by (1)H-NMR and (13)C-NMR. Therefore, the RSM was effective to optimize the preparation of 20(R)-ginsenoside Rg3 by converting PPD saponins using d, l-tartaric acid.

摘要

采用基于三因素六水平中心组合设计的响应面法(RSM),对利用市售的 d,l-酒石酸优化选择性制备 20(R)-人参皂苷 Rg3 转化原人参二醇型皂苷(PPD 皂苷)的条件进行了优化。通过最大响应的典型分析,预测在因素(d,l-酒石酸浓度 1.19mol/L、温度 107.9°C 和时间 2.79h)的组合下,20(R)-人参皂苷 Rg3 的最优脱%为 94.52%。在最佳反应条件下,实际的 20(R)-人参皂苷 Rg3 的脱%为 96.49%。通过 (1)H-NMR 和 (13)C-NMR 分离和鉴定了 20(R)-人参皂苷 Rg3(1)和 20(S)-人参皂苷 Rg3(2)。因此,RSM 可有效优化利用 d,l-酒石酸转化 PPD 皂苷制备 20(R)-人参皂苷 Rg3。

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