An eight-step gram-scale synthesis of (-)-jiadifenolide
An eight-step gram-scale synthesis of (-)-jiadifenolide
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DOI：
10.1038/nchem.2283
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发表时间：
2015-07-01
期刊：
影响因子：
21.8
通讯作者：
Shenvi, Ryan A.
中科院分区：
文献类型：
--
作者：
Lu, Hai-Hua;Martinez, Michael D.;Shenvi, Ryan A.
将具有生物活性的次级代谢物开发成有用的药物需要持续获得大量的材料。尽管任何化学合成都因其多功能性而广泛有用，但确定一种可以经济地扩展的合成路线代表着更大的挑战。在这里，我们报告了神经营养微量代谢物(-)-甲地酚内酯的简明合成及其在克级上的生产。该路线的简便性和许多有效的八头藤萜的关键中间体的结构相似性使化学合成成为获得和修饰这些潜在治疗药物的无可争议的方法。
Development of a biologically active secondary metabolite into a useful medicine requires continuous access to meaningful quantities of material. Although any chemical synthesis is broadly useful for its versatility, identification of a synthesis route that can be economically scaled represents a greater challenge. Here we report a concise synthesis of the neurotrophic trace metabolite (-)-jiadifenolide and its production on a gram-scale. The brevity of the route and the structural similarity of a key intermediate to many potent Illicium terpenes make chemical synthesis the unquestionable method for accessing and modifying these potential therapeutics.