Catalytic Methods for Rapid Aromatic Derivatization

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Project Summary The objective of this research proposal is to develop new catalytic protocols for the direct C–H functionalization of aromatic compounds. Aromatic compounds are central motifs in the vast majority of therapeutics and simple methods for their further elaboration are always in demand. The goal of this research program is to generate new synthetic tools for biomedical researchers to be able to derivatize lead aromatic-containing therapeutics in order to assemble libraries of drug candidates for further evaluation. This proposal describes the use of organic dyes as catalysts to enable over a dozen new chemical transformations. The value of the proposed synthetic methods is the ability to utilize aromatics that are not pre-oxidized, allowing for greater flexibility in the types of aromatic structures that can be employed. We predict that this research program will enhance the synthetic capabilities of medicinal chemists to explore greater chemical space in the development of small molecule therapeutics.