LCMS Equipment For Diversity Oriented Synthesis, New Microarray Technology and New Synthetic Methodology

这份资助申请是用于一种叫做“液相色谱-质谱仪”（LCMS）的分析仪器。该设备可以快速分析小分子样品，这对于有机合成中的高通量表征至关重要。该工具将支持的研究的共同主题涉及开发新的方法和技术，以发现和合成生物活性小分子，如新的药物。该仪器将直接支持两个特定方面的研究：新的合成方法/包括多样性导向合成，有机催化，C-H活化新的高通量合成技术/小分子微阵列多样性导向合成是有机合成中的一个新概念，其目的是有效地合成结构多样性小分子的集合。我们将进行以多样性为导向的合成，以获得迄今为止具有最高结构多样性的产品。通过简单的催化方法制备对映体纯分子的能力是现代有机合成的关键目标。对映选择性有机催化是一种新的手性分子组装方法，我们的目标是开发新的反应和催化剂，从而为化学合成提供一个通用的范例。金属催化的C-H键活化涉及到将特定的惰性C-H键官能化为有用分子的能力。我们计划设计新的工艺，打破传统的键断，为复杂的分子合成带来创新和新颖的方法。最先进的生产，储存和生物测试一百万个药物样分子是昂贵的，需要几个月，如果不是几年;然而，如果我们开创性的微阵列技术的愿景得以实现，然后，通过以更小、更快和更便宜的形式“按需”制造和测试小分子，这一过程将发生革命性变化。我们相信，所要求的LCMS具有成本效益，为现有的EPSRC/资助研究增加了巨大的价值，对于科普研究成果至关重要，并且对于我们的研究彻底改变小分子合成的真正潜力是绝对至关重要的。

This grant application is for an analytical instrument called a 'liquid chromatography-mass spectrometer' (LCMS). The equipment permits a rapid analysis of small molecule samples, which is essential for high throughput characterization in organic synthesis. The common theme of the research that this instrument will support concerns the development of new approaches and techniques to discover and synthesize bioactive small molecules, such as new pharmaceutical drugs. There are two particular aspects of the research that this instrument will support directly:New synthetic methodology / including diversity-oriented synthesis, organocatalysis, C-H activationNew high throughput synthesis technology / small molecule microarraysDiversity-oriented synthesis is a new concept in organic synthesis, where the aim is to synthesize collections of structurally-diverse small molecules efficiently. We will perform a diversity-oriented synthesis to give products with the highest range of structural diversity to date. The ability to make enantiopure molecules by facile catalytic methods is a key objective in modern organic synthesis. Enantioselective organocatalysis represents an exciting new method by which chiral molecules can be readily assembled and we aim to develop new reactions and catalysts that will lead to a general paradigm in chemical synthesis.Metal catalyzed C-H activation relates to the ability to functionalize a specific, supposedly inert, C-H bond to a useful molecule. We plan to design new processes that break away from the traditional bond disconnections leading to innovative and novel methods for complex molecule synthesis.State-of-the-art production, storage and biological testing of a million drug-like molecules is expensive and takes months if not years; however, if the vision of our pioneering microarray technology is realized, then this process will be revolutionized by making and testing small molecules 'on-demand' in a smaller, faster and cheaper format.We believe that the LCMS requested is cost-effective, adds enormous value to existing EPSRC/funded research, is vital to cope with research output, and is absolutely crucial to deliver the true potential of our research to revolutionize small molecule synthesis.