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Transition-Metal-Catalysed Cycloaddition Methodology for the Convergent Assembly of (Hetero)Aromatic Compounds

用于（杂）芳香族化合物聚合组装的过渡金属催化环加成方法

基本信息

批准号：
EP/F068190/1
负责人：
Hon Lam
金额：
$ 34.59万
依托单位：
University of Edinburgh
依托单位国家：
英国
项目类别：
Research Grant
财政年份：
2008
资助国家：
英国
起止时间：
2008 至无数据
项目状态：
已结题

来源：
https://gtr.ukri.org/projects?ref=EP%2FF068190%2F1
关键词：
Transition Metal Catalysed Cycloaddition Methodology

项目摘要

The continued development of new medicines by the pharmaceutical industry is a critical endeavour to improve and maintain human health, and the associated benefits to society are obvious. In order to develop new drugs, pharmaceutical chemists must prepare large collections of diverse compounds in order to identify a promising hit , which is then taken on for further development in the production of further collections of compounds. Therefore, as one might imagine, the methods (chemical reactions) which are used to prepare these compounds must be very efficient, reliable, and general in nature.Although a huge number of chemical reactions are known, (a number that continues to grow on a daily basis), only a very small proportion of these reactions are suitable for use in the preparation of these compound libraries. This is because most reactions fail to meet one or more of a list of demanding criteria that are applied in the generation of compound libraries. For example, many reactions only work for a narrow, restricted range of cases, or they require the use of exotic reagents or inconvenient reaction conditions. This limiting factor provides a powerful obstacle to the efficient development of new medicines.The proposed research is aimed at developing a reaction that has been known for a long time, but is rarely used by medicinal chemists in the pharmaceutical industry. This reaction employs a transition-metal catalyst to promote the reaction between several reaction partners to generate cyclic molecules that feature prominently in drugs and drug-like molecules. We will develop new variants of the general methodologies specifically targeted at the requirements of medicinal chemists, as well as modifying existing methodologies that currently do not quite fit these requirements. We anticipate that we can make numerous advances to positively impact the process of drug discovery, developing valuable (and publishable) chemistries along the way.This research will be conducted by a postdoctoral research associate working jointly at the University of Edinburgh and at GlaxoSmithKline, where they will have access to state-of-the-art equipment.

制药行业持续开发新药是改善和维护人类健康的重要努力，给社会带来的好处是显而易见的。为了开发新药，药物化学家必须制备大量不同的化合物，以确定有希望的药物，然后将其用于进一步开发，生产更多化合物。因此，正如人们所想象的那样，用于制备这些化合物的方法（化学反应）必须非常高效、可靠且通用。尽管已知大量的化学反应（数量每天都在持续增长），但这些反应中只有极少数适合用于制备这些化合物库。这是因为大多数反应无法满足在生成化合物库时应用的一系列严格标准中的一个或多个。例如，许多反应仅适用于狭窄、受限的情况，或者需要使用外来试剂或不方便的反应条件。这一限制因素为新药的有效开发提供了强大的障碍。本次研究旨在开发一种早已为人所知、但在制药行业中很少被药物化学家使用的反应。该反应采用过渡金属催化剂来促进多个反应伙伴之间的反应，从而生成在药物和类药物分子中具有显着特征的环状分子。我们将专门针对药物化学家的要求开发一般方法的新变体，并修改目前不太符合这些要求的现有方法。我们预计我们可以取得许多进展，对药物发现过程产生积极影响，一路开发有价值的（且可发表的）化学物质。这项研究将由爱丁堡大学和葛兰素史克联合工作的博士后研究员进行，他们将在那里使用最先进的设备。