药学学报, 2011, 46(12): 1471-1475
引用本文:
张天才, 叶鹤琳, 柳军玺, 邸多隆. 天然产物异紫堇二酮的半合成转化研究[J]. 药学学报, 2011, 46(12): 1471-1475.
ZHANG Tian-cai, YE He-lin, LIU Jun-xi, DI Duo-long. Study on semi-synthetic transforming technology for the natural product of isocorydione[J]. Acta Pharmaceutica Sinica, 2011, 46(12): 1471-1475.

天然产物异紫堇二酮的半合成转化研究
张天才1, 2, 叶鹤琳2, 柳军玺2*, 邸多隆1, 2*
(1. 甘肃中医学院药学系, 甘肃 兰州 730000; 2. 中国科学院兰州化学物理研究所, 中国科学院西北特色植物资源化学重点实验室, 甘肃省天然药物重点实验室, 甘肃 兰州 730000)
摘要:

通过紫外分光光度法, 以异紫堇二酮的半合成转化产率为指标, 详细考察反应时间、反应温度和投料比 (异紫堇碱弗瑞米自由基) 对转化产率的影响, 确定异紫堇二酮的最佳合成条件: pH值为10的磷酸氢二钠溶液为反应介质、反应温度25 、投料比 (异紫堇碱弗瑞米自由基) = 12, 反应时间12 h, 通过氧化异紫堇碱可以半合成转化制备异紫堇二酮, 产率可达到50.0%, 并首次通过X-ray单晶衍射测定异紫堇二酮的化学结构。

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Study on semi-synthetic transforming technology for the natural product of isocorydione
Abstract:

Transforming technology for semi-synthesized isocorydione from the natural product of isocorydine was studied.  The factors affecting on the reaction yield were investigated.  UV spectrophotometry was used to indicate the semi-synthesized yield of isocorydione.  The optimum reaction conditions were determined as following: reacting for 12 h in the solution of sodium dihydrogen phosphate at pH 10, the temperature was 25 and the ratio of isocorydine to Fremy’s radical was 12.  Under the optimum conditions, the yield could reach up to 50.0%.  The molecular structure of isocorydione was elucidated by X-ray single-crystal diffraction analysis for the first time.

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