A study for the common synthetic method to biologically active indole alkaloids and for the creation of our own leads compounds

我们打开了“1-羟基吲哚化学”这一处女地的新大门，并将其确立为日本的知识产权。在扩展化学的过程中，我们有了各种新发现和新反应。1-羟基吲哚的产生我们已经产生了各种迄今未知的新的1-羟基吲哚化合物。特别是，1-羟基色氨酸和-色胺衍生物是重要的。它们在吲哚氮上发生亲核取代反应。1-羟基褪黑素二聚化的发现。该反应成功制备了3a，3a'-双吡咯[2,3-b]吲哚核。这一新的反应已被尝试用于合成具有生物活性的鱿鱼吲哚生物碱，有望成为治疗阿尔茨海默病的先导化合物。合成现在已进入最后阶段。多核上的亲核取代反应这是首次发现的前所未有的新反应。应用这些反应，包括2-取代吲哚在内的各种构建模块，迄今为止难以通过传统化学方法获得，变得很容易获得。

We have opened the new door to the virgin territory of "the chemistry of 1-hydroxyindoles" and established it as an intellectual property of Japan. In the course of extending the chemistry, we have developed various new findings and new reactions.1.Creation of 1-HydroxyindolesWe have given birth to various new 1-hydroxyindole compounds thus far unknown. Especially, 1-hydroxy-tryptophan and -tryptamine derivatives are important. They undergo nucleophilic substitution reactions on the indole nitrogen.2.Discovery of dimerization of 1-hydroxymelatonin.The reaction was applied successfully to make 3a,3a'-bispyrrolo[2,3-b]indole nucleus. This new reaction has been attempted to apply for the synthesis of biologically active calabar indole alkaloids, which are expected to be lead compounds for Altzheimer's diseases. The synthesis is now in the final stage.3.Nucleophilic substitution reactions on in dole nucleusThis unprecedented new reactions are discovered for the first time. Applying the reactions, various kinds of building blocks, including 2-substituted indoles, thus far hardly accessible by the conventional chemistry, become readily available.