New array strategies using C-H borylation chemistry

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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.