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.

分子的结构和形状取决于原子如何连接在一起。原子之间化学键的形成是制造分子的基本过程。具有潜在药用重要性的有机分子的合成几乎完全取决于碳原子之间的化学键形成。碳原子之间键的形成不会自发发生，通常需要两个活化的摩尔孔的正确结合。为了激活分子，有必要对其进行化学修饰（例如，在其上添加激活的摩尔孔）。尽管此过程需要额外的化学反应，从而降低了该过程的总体效率。此外，在进行所需的债券形成后，您将留下对任何人无用的残留激活剂。此外，这些残留物通常是有毒的，并且处置可能很昂贵。因此，当前的C-C键形成方法通常效率低下，可以描述为原子经济差（即，您在起始分子中使用的原子并不多的原子最终出现在新分子中）。本质上最常见的键是C-H键，并且通常将其分类为无反应性（除非它们接近活性功能组）。从概念上讲，如果您可以从简单的C-H键中建立重要的C-C键，那么您将损失的只是两个氢原子。这种原子不仅是原子经济（H2的分子质量为2，这是产品质量的一小部分）。因此，如果我们可以从C-H债券中形成C-C键，那么您不必预先激活，而且几乎不会失去任何东西。它使整个过程效率更高，环保和成本效益。这项研究涉及试图通过简单地激活“惰性” C-H键来发现具有重要药用特性（例如抗癌）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。因为这是一个新领域，因此发现您甚至没有寻找的东西，当然也可能导致全新的研究领域。归根结底，这是发现可能在日常生活中产生重要后果的新事物的兴奋，这会推动科学前进。该提案最近是通过响应模式提交的，尽管没有资助，但建议立即重新提取6个月的延迟。该提案并未与原始提案更改。