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

Lead Research Organisation: University of Cambridge
Department Name: Chemistry


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.


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Nicholson RL (2007) Fluorous tagged small molecule microarrays. in Chemical communications (Cambridge, England)

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Phipps RJ (2009) A meta-selective copper-catalyzed C-H bond arylation. in Science (New York, N.Y.)

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Thomas GL (2008) Anti-MRSA agent discovery using diversity-oriented synthesis. in Angewandte Chemie (International ed. in English)

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Vo NT (2008) An enantioselective organocatalytic oxidative dearomatization strategy. in Journal of the American Chemical Society

Description The equipment has been essential for the success of all projects in the collaborating groups in Cambridge. This has included the discovery of new antibacterial molecules, micro arraying technologies and new synthetic methodology.
Exploitation Route The equipment has been used by many groups and researchers in Cambridge.
Sectors Chemicals

Description In shaping the field of chemistry we are researching, and in the area of drug discovery strategies more broadly.
First Year Of Impact 2011
Sector Chemicals,Pharmaceuticals and Medical Biotechnology
Impact Types Economic