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雷公藤内酯醇(triptolide)[Ⅰ]是从卫矛科雷公藤属植物雷公藤(Triptery gium wilfordii Hook. F)中分离到的二萜内酯化合物,药理试验具有抗白血病活性,临床已试用于治疗白血病。因为原植物中[Ⅰ]的含量很低,我们将在分离[Ⅰ]的过程中得到雷公藤内酯酮(triptonide)[Ⅲ),用四氢硼钠进行还原反应,产物经硅胶柱层析分离,得到[Ⅰ](24%)和14-表雷公藤内酯醇(14-epit riptolide)[Ⅱ](72%)。虽然化学转化的结果[Ⅰ]的量较低,但没有抗白血病活性的[Ⅱ]又可以用吡啶重铬酸盐(2PgH~((+))Cr_2O_7~(2(-))氧化,得到高产率的[Ⅲ](80%)。
Triptolide [I] is a diterpene lactone compound isolated from Triptery gium wilfordii Hook. F. It has anti-leukemia activity and has been clinically tested. Treatment of leukemia. Because the content of [I] in the original plant is very low, we will obtain triptonide [III] during the separation of [I], and use sodium tetrahydroborate for reduction. The product is separated by silica gel column chromatography. Obtained [I] (24%) and 14-epitriptonide [II] (72%). Although the amount of chemical conversion [I] is low, [II] without anti-leukemia activity can be oxidized with pyridine dichromate (2PgH((+))Cr_2O_7~(2(-)) to yield high yields. The rate of [III] (80%).