The advances in C-H functionalization have led to the development of new methods to conveniently install functional groups in organic molecules. Since aromatics are a prominent motif in pharmaceuticals, creating a simple method for the post-synthetic modification of aryl moieties could allow for the streamlined derivatization of potential drug candidates. Derivatization of arenes tends to rely on metal mediated C-H activation approaches or harsh reaction conditions. In our lab, we have developed a mild method to halogenate and oxygenate arenes with para-selectivity. Our synthetic approach can successfully functionalize a wide range of aromatics and heterocycles including anilides, anisoles, (iso)quinolines, pyridines, and pyrimidines.

Para-selective halogenation and oxygenation of arenes

253rd National Meeting (2017)

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