【摘 要】
:
卡马拉素(rottlerin)是一种不对称的乙酰间苯三酚衍生物,存在于植物Mallotus philippensis的果实中,该天然产物具有抗肿瘤、调控自吞噬等多种生物作用。目前卡马拉素的主要来源是从卡马拉果实中提取,但是由于它不稳定性以及高昂的价格和提取纯度低,严重影响了其进一步的生物活性研究。基于上述问题,我们本着高效实用的原则,从易得价廉的原料出发,通过7步总收率47%克级制备rottler
【机 构】
:
中国科学院上海有机化学研究所,上海市,200032 中国科学院上海有机化学研究所,上海市,2000
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卡马拉素(rottlerin)是一种不对称的乙酰间苯三酚衍生物,存在于植物Mallotus philippensis的果实中,该天然产物具有抗肿瘤、调控自吞噬等多种生物作用。目前卡马拉素的主要来源是从卡马拉果实中提取,但是由于它不稳定性以及高昂的价格和提取纯度低,严重影响了其进一步的生物活性研究。基于上述问题,我们本着高效实用的原则,从易得价廉的原料出发,通过7步总收率47%克级制备rottlerin右边片段(6),以3步总收率67%克级制备rottlerin左边片段(4),最后反应条件筛选,用37%甲醛溶液为亚甲基试剂,浓硫酸作为质子酸,通过酚醛缩合反应成功合成rottlerin,实现了总步骤11步最长线性步骤8步20%总产率高效合成该天然产物。我们的工作为实验室获得高纯度rottlerin提供了一种可行的合成方法。
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