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

Development of novel strategies towards the synthesis of N-heterocycles using isocyanide-based multicomponent reactions
利用基于异氰化物的多组分反应开发合成 N-杂环的新策略
批准号:
245024820
负责人:
Professor Dr. Stefan Bräse
金额:
$0.0万
依托单位国家:
德国
项目类别:
Research Grants
财政年份:
2014
资助国家:
德国
项目状态:
已结题
起止时间:
2013-12-31 至 2017-12-31

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中文摘要
翻译
我们在日常生活的许多领域都遇到有机化学的杂环化合物。此外,它们使人类的生命成为可能,因为它们是核酸、ATP或血红蛋白的组成部分。此外,杂环化合物还存在于食物和营养品(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,它们被用作抗炎、抗肿瘤、镇痛或抗生素剂。一个众所周知的例子是青霉素化合物。制药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的副作用。目的是用一种简单快速的方法合成不同功能的杂环化合物。同时,形成的构造具有高度的复杂性和多样性。由此产生的化合物库可以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。除了反应顺序快速高效外,MCR还具有资源可持续利用的优势。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这种新的多组分反应,以异氰化物为基础合成N杂环。这一特殊的合作努力不仅体现在印度和德国之间的知识交流,而且体现在两种技术之间,即液相组合化学与固相组合化学。最后,将对合成的化合物进行初步的体外和体内生物筛选。
英文摘要
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.
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