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

具有生物活性的吲哚生物碱的常见合成方法以及我们自己的先导化合物的创建的研究

基本信息

批准号：
15590002
负责人：
SOMEI Masanori
金额：
$ 2.3万
依托单位：
Kanazawa University
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (C)
财政年份：
2003
资助国家：
日本
起止时间：
2003 至 2004
项目状态：
已结题

项目摘要

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.

我们已经打开了新的大门“1-羟基吲哚化学”的处女地，并将其确立为日本的知识产权。1. 1-羟基吲哚的合成我们已经合成了许多新的1-羟基吲哚化合物，这些化合物至今还不为人所知。特别是，1-羟基-色氨酸和-色胺衍生物是重要的。2.发现了1-羟基褪黑激素的二聚化反应，成功地合成了3a，3a '-双吡咯并[2，3-B]吲哚核。这一新反应已被尝试应用于合成具有生物活性的卡拉巴吲哚生物碱，这些生物碱有望成为治疗阿尔茨海默病的先导化合物。3.多尔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，迄今为止难以通过常规化学获得的各种结构单元，包括2-取代的吲哚，变得容易获得。