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Concise synthesis of the bioactive natural polyhydroxynaphthoate parvinaphthol B via Hauser-Kraus annulation
Tetrahedron Letters ( IF 1.8 ) Pub Date : 2017-11-11 , DOI: 10.1016/j.tetlet.2017.11.024
Sungwan Ahn , Young Taek Han

Herein, we describe the first total synthesis of parvinaphthol B, a polyhydroxynaphthoate derived from the root of Pentas parvifolia which exhibits cytotoxic effects against the TNBC cell line. The key feature of the synthesis involves a Hauser-Kraus annulation to provide the polyhydroxynaphthoate skeleton. The synthesis requires only six linear steps and afforded the product in 26.5% overall yield, thus representing a simple method for the further preparation of analogs and biological studies.



中文翻译:

通过豪瑟尔-克劳斯(Hauser-Kraus)环空法合成生物活性天然多羟基萘甲酸小萘酚B

此,我们描述parvinaphthol B,从根衍生的polyhydroxynaphthoate的第一全合成繁星小叶其表现出针对TNBC细胞系细胞毒性效应。合成的关键特征涉及Hauser-Kraus环空法,以提供聚羟基萘甲酸酯骨架。合成仅需六个线性步骤,即可以26.5%的总收率获得产物,因此代表了一种用于进一步制备类似物和生物学研究的简单方法。

更新日期:2017-11-11
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