New Technology for Chemical Synthesis via Metal Catalysed C-H Functionalisation
New Technology for Chemical Synthesis via Metal Catalysed C-H Functionalisation
批准号:
EP/D078180/1
负责人:
Matthew Gaunt
金额:
$39.15万
依托单位:
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
项目状态:
已结题
起止时间:
2006 至 --
中文摘要
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分子形成的基本过程。具有潜在药用价值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。碳原子之间的键不是自发形成的,它们通常需要两个活化分子的正确结合。为了激活分子,必须对其进行化学修饰(例如向其添加激活分子)。这个过程需要一个额外的化学反应,从而降低了整个过程的效率。此外,在所需的键形成完成后,剩下的活化剂对任何人都没有用处。此外,这些残留物通常是有毒的,处理起来也很昂贵。因此,目前的碳碳键形成方法往往效率低下,可以描述为具有较差的原子经济性(即。在开始的分子中使用的原子很少最终会变成新的分子)。自然界中最常见的键是碳氢键,这些键通常被归类为非活性键(除非它们靠近激活官能团)。从概念上讲,如果你能从简单的碳氢键变成一个重要的碳碳键那么你失去的只是两个氢原子。这个原子不仅经济(H2的分子质量是2,这只是产物质量的一小部分)。因此,如果我们能从碳氢键形成碳碳键就不需要预激活也几乎不会损失任何东西。它使整个过程更加高效、环保和经济。这项研究试图发现通过激活“惰性”碳氢键来制造具有重要药用特性(如抗癌)的分子的新方法。它使合成化学家能够快速有效地制造这些重要的结构,从而加快药物发现过程。因为这是一个全新的领域,所以也有可能发现一些你从未寻找过的东西,当然,这可以引导你进入全新的研究领域。在一天结束的时候,正是发现可能对日常生活产生重要影响的新事物的兴奋推动着科学向前发展。该提案最近通过响应模式提交,虽然没有获得资助,但建议立即重新提交,并放弃6个月的延迟。这个建议与原来的没有变化。
英文摘要
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.
期刊论文(4)
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