Abstract

A Cu-catalyzed regioselective C5-H arylation of imidazo[1,5-a]pyridines with aryl iodides was achieved with the assistance of an ethylthio group at the C3 position. This directing group could be easily removed to furnish a range of 5-(hetero)arylimidazo[1,5-a]pyridine derivatives. The reaction tolerates a variety of functionalities and is compatible with sterically hindered substrates.

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