N-alkylation of 2-pyridone derivatives via palladium(II)-catalyzed directed alkene hydroamination

Add time:08/09/2019    Source:sciencedirect.com

A selective N-alkylation reaction of 2-pyridones and related heterocycles via intermolecular alkene hydroamination is reported. The reaction utilizes palladium(II) acetate as a catalyst and employs a bidentate directing group to dictate the regioselectivity for both unactivated terminal and internal alkenes. High functional group tolerance is observed across a widerange of electronically diverse 2-pyridones and other aza-heterocycles, including 1-hydroxyisoquinoline, 2-hydroxyquinoline, pyridazinone, pyrimidinone, and pyrazinone.

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