Development of novel strategies towards the synthesis of N-heterocycles using isocyanide-based multicomponent reactions

我们在日常生活的许多领域都会遇到有机杂环化合物。此外，它们使人类的生命成为可能，因为它们是核酸、三磷酸腺苷或血红蛋白的组成部分。此外，杂环还存在于食物和营养物质(咖啡因、维生素)或不同种类的染料中。然而，杂环化合物最大的应用领域是制药工业，在那里它们被用作抗炎、抗肿瘤、止痛或抗生素。一个广为人知的例子是复方青霉素。药物和有机化学的一个主要目标是进一步开发这类药物，从而提高其有效性或减少不良反应。目的是用一种简单快速的技术合成不同的功能杂环。同时，形成的构造要达到高度的复杂性和多样性。由此得到的化合物文库使得能够快速发现合适的活性成分。为此，多组分反应是一种特别有前途的合成方法。除了快速高效的反应顺序外，MCR还具有可持续利用资源的优势。基于双方在双边国际合作中的初步工作，该项目的目标是开发基于异氰化物合成N杂环的这种新的多组分反应。特别的合作努力不仅体现在印度和德国的知识交流上，而且还体现在两种技术之间，即液相组合化学和固相组合化学之间。最后，合成的化合物将在初步的体外和体内生物筛选中进行探索。

We encounter heterocyclic compounds of organic chemistry in many areas of daily life. Furthermore, they make human life possible, as they are components of nucleic acids, ATP, or hemoglobin. Moreover, heterocycles are found in food and nutrition (caffeine, vitamins) or in different kinds of dyes. However, the largest field of application for heterocyclic compounds is the pharmaceutical industry, where they are used as anti-inflammatory, antitumor, analgesic or antibiotic agents. A well-known example is the compound penicillin. A major goal of pharmaceutical and organic chemistry is to further develop such kind of drugs and thereby enhance their effectivity or reduce undesirable side effects. The aim is the synthesis of different functional heterocycles using a simple and fast technique. Simultaneously a high degree of complexity and diversity of the formed constructs is to be achieved. The resulting compound libraries thus enable the rapid discovery of suitable active components. For such purpose, the multi-component reaction is a particularly promising synthetic method. In addition to the fast and efficient reaction sequence, the MCR has also the advantage of a sustainable use of resources. Founded on preliminary work of both partners in this bilateral international cooperation, the goal of this project is the development of such new multicomponent reactions for the synthesis of N heterocycles based on the use of isocyanides.The special collaborative effort is exemplified by a knowledge exchange not only from India and Germany, but also between two techniques i.e. liquid phase combinatorial chemistry versus solid phase combinatorial chemistry. Lastly, the compounds synthesized will be explored in initial in-vitro and in-vivo biological screens.