New array strategies using C-H borylation chemistry

Lead Research Organisation: Durham University
Department Name: Chemistry


In order to evaluate and optimise (small) molecules for a particular function, e.g. as a drug molecule, it is necessary to prepare a range of analogues that differ in structure. This is known as an array and the efficient synthesis of such arrays requires reactions that can be used on multiple samples simultaneously. The variety of chemical reactions currently used in array preparation is limited and the research in this project is designed to address this need based on chemistry of the boronic acid functional group. In particular we will develop new array synthetic strategies using direct catalytic C-H borylation chemistry. This requires evaluation of new substrate classes and an optimisation of the catalysts to give better selectivity and reactivity. This will provide sets of new boronic acids from unfunctionalised aromatic and heteroaromatic precursors. In addition, the boronic acids are themselves used in many synthetic transformations and we will explore using the arrays of boronic acids as starting points for a further generation of array synthesis.


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Description C-H borylation can be an efficient method for the late stage generation of analogues of drug like molecules - pharmaceutical leads
Exploitation Route similar transformations are now being used in other drug discovery programmes
Sectors Pharmaceuticals and Medical Biotechnology

Description used at GSK by DU researcher on placement to explore library enrichment strategies - reported in primary literature
First Year Of Impact 2012
Sector Pharmaceuticals and Medical Biotechnology
Description Astra Zeneca Case Award
Amount £24,000 (GBP)
Organisation AstraZeneca 
Sector Private
Country United Kingdom
Start 09/2012 
End 09/2015
Description CASE collaboration with GSK 
Organisation GlaxoSmithKline (GSK)
Country Global 
Sector Private 
PI Contribution Academic research results
Collaborator Contribution Intellectual input - Industrial supervision - industrial secondment
Impact None yet
Start Year 2013