New Technology for Chemical Synthesis via Metal Catalysed C-H Functionalisation

金属催化C-H官能化化学合成新技术

• 批准号: EP/D078180/1
• 负责人: Matthew Gaunt
• 金额: $ 39.15万
• 依托单位: University of Cambridge
• 依托单位国家: 英国
• 项目类别: Research Grant
• 财政年份: 2006
• 资助国家: 英国
• 起止时间: 2006 至 无数据
• 项目状态: 已结题
• 来源: https://gtr.ukri.org/projects?ref=EP%2FD078180%2F1
• 关键词: New; Technology; Chemical; Synthesis; via

The structure and shape of molecules is determined by how atoms are joined together. The formation of chemical bonds between atoms is a fundamental process for making molecules. The synthesis of organic molecules that are of potential medicinal importance relies almost exclusively on the formation of chemical bonds between carbon atoms. The formation of bonds between carbon atoms does not happen spontaneously, they usually require the correct union of two activated moelcules. In order to activate the molecule it is necessary to chemically modifiy it (for example add an activating moelcule to it). This process though requires an additional chemcial reaction and thus reducues the overall efficiency of the process. Furthermore, after the desired bond formation is carried out you are left with the residual activating agent that is of no use to anyone. Furthermore, these residues are often toxic and can be expensive to dispose of. Therefore, current methods of C-C bond formation are often inefficient and can be described as having poor atom economy (ie. not many of the atoms that you use in the starting molecules end up in the new molecule).The most common bond in nature is the C-H bond, and these are usually classed as unreactive (unless they are close to an activating functional group). Conceptually, if you can make an important C-C bond from simple C-H bond then all you lose are two hydrogen atoms. Not only is this atom economic (H2 has a molecular mass of 2 and this is a tiny fraction of the product mass). Therefore, if we can form C-C bonds from C-H bonds then you don't have to preactivate and you hardly lose anything. It makes the whole process more efficient, environmentally friendly and cost efficient. This research involves trying to discover new ways to make molecules that have important medicinal properties (like anti-cancer) by simply activating 'inert' C-H bonds. It allows the synthetic chemist to make these important structures quickly and efficiently that can speed up the drug discovery process. Becasue this is such a new area there is also the possibility if discovering things that you weren't even looking for and of course this can lead into whole new areas of research. At the end of the day it is the excitment of discovering something new that might have important consequences in everyday life that drives science forward. This proposal was recently submitted through responsive mode and although was not funded was recommended for immediate re-submission with the 6-month delay waived. The proposal has not changed from the original.

分子的结构和形状是由原子如何结合在一起决定的。原子间化学键的形成是制造分子的基本过程。具有潜在医学重要性的有机分子的合成几乎完全依赖于碳原子之间化学键的形成。碳原子之间的键的形成不是自发发生的，它们通常需要两个活化分子的正确结合。为了激活分子，有必要对其进行化学修饰（例如向其添加活化分子）。然而，该方法需要额外的化学反应，因此降低了该方法的总体效率。此外，在进行所需的键合形成之后，留下对任何人都没有用的残余活化剂。此外，这些残留物通常是有毒的，处理起来可能很昂贵。因此，目前的C-C键形成方法通常是低效的，并且可以被描述为具有差的原子经济性（即，在自然界中最常见的键是C-H键，这些键通常被归类为不反应的（除非它们靠近活化官能团）。从概念上讲，如果你能从简单的C-H键，合成一个重要的C-C键，那么你失去的只是两个氢原子。这个原子不仅经济（H2的分子量为2，这是产品质量的一小部分）。因此，如果我们能从C-H键形成C-C键，那么你就不需要预先激活，你几乎不会失去任何东西。它使整个过程更加高效，环保和具有成本效益。这项研究试图通过简单地激活“惰性”C-H键来发现制造具有重要药用特性（如抗癌）的分子的新方法。它允许合成化学家快速有效地制造这些重要的结构，从而加快药物发现过程。因为这是一个新的领域，如果发现你甚至没有寻找的东西，当然这可能会导致全新的研究领域。在一天结束的时候，是发现新事物的兴奋，这些新事物可能会对日常生活产生重要影响，从而推动科学向前发展。该提案是最近通过响应模式提交的，虽然没有得到资助，但建议立即重新提交，取消6个月的延迟。该建议与原来的建议没有变化。