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癸酰乙醛(n-壬基-β-酮醛)为清热解毒中草药鱼腥草的有效成分之一,其亚硫酸氢钠加成物(鱼腥草素)已在临床上用为抗菌消炎药物。这一事实导致我们合成了一些癸酰乙醛衍生物,目的为寻找更有效的抗病毒、抗菌药物。其中鱼腥草素异菸腙虽无抗病毒作用,但在体内、体外皆具有显著的抗结核活性,初步临床试验亦证明有一定的治疗效果。 将甲壬酮与甲酸乙酯在金属钠存在下在无水苯中反应,形成的β-酮醛与相应的氨基化合物缩合,即获得所需要的最终产物。
Decanoyl acetaldehyde (n-nonyl-β-ketoaldehyde) is one of the active ingredients of Chinese Herb Houttuynia Cordata, its sodium bisulfite adduct (houttuynin) has been clinically used for anti-bacterial anti-inflammatory drug. The fact that we have led to the synthesis of some decanoyl acetaldehyde derivatives, the purpose of finding more effective anti-virus, anti-bacterial drugs. Houttuynin isoniazid has no anti-virus effect, but has significant antituberculous activity both in vivo and in vitro. Preliminary clinical trials have also proved that there is a certain therapeutic effect. The reaction of p-nonanone with ethyl formate in anhydrous benzene in the presence of sodium metal yields the condensation of the resulting β-ketoaldehyde with the corresponding amino compound to provide the desired final product.