Synthesis of Bioactive Anthraquinones Using Intramolecular

近年来，已有报道具有许多有趣的活性，如神经细胞保护活性(Espicufolin)、抗螺旋体活性(AH-1763 IIa)和碳清除活性(SS43405E)。在本研究中，我们完成了七叶皂苷的合成和绝对结构测定，完成了SS43405E的合成和绝对结构测定，建立了以K1115A为代表的二羟基蒽醌类化合物的合成路线。用小鼠胚胎神经细胞对外消旋和S-七叶皂苷进行了生物测定。灯盏细辛对谷氨酸的毒性无保护作用，但对供试细胞有微弱的细胞毒作用。在抗螺旋体AH-1763 IIa的合成方法中，研究了两条不同的路线，但尚未实现全合成。我们现在打算通过不对称的羟醛缩合反应制备AH-1763 IIa的侧链。

Recently, compounds with an anthraquinone skeleton have been reported to have many interesting activities such as neuronal cell-protecting activity (espicufolin), anti-helpetic activity (AH-1763 IIa), and carbon clearance activity (SS43405E). We planned not only to prepare the bioactive anthraquinones and their analogs, but also to create highly active compounds by elucidation of their in vivo action mechanisms on neuronal cells.In this research, we achieved the synthesis and absolute structure determination of espicufolin, the synthesis and absolute structure determination of SS43405E, and establishment of the synthetic routes to dihydroxyanthraquinones represented by K1115A. Racemic and S-espicfolins were subject to bioassay by using mouse embryonic neuronal cells. The espicufolins showed no protecting activity for the toxicity of glutamate but weak cytotoxiciry to the cells employed. In the synthetic approach for antihelpetic AH-1763 IIa, two different routes were examined, but total synthesis has not been achieved, yet. We now intended to prepare the side chain of AH-1763 IIa by asymmetric aldol condensation.