Abstract
AbstractWe report herein a catalytic synthetic method for enantioenrichedN‐substituted pyridones. By employing chiral iridium catalyst generated from the Carreira [P/olefin] ligand, intermolecular asymmetric allylic amination of allyl alcohols with pyridones proceeded smoothly with excellent chemo‐, regio‐ and enantioselectivities (>19:1N/O, >19:1 b/l and ≥89% ee). The reaction was a kinetic resolution process under mild conditions and displayed a broad substrate scope for both pyridones and allylic alcohols. The potential of this method was demonstrated by a gram‐scale reaction with only 0.6 mol% catalyst loading and diverse transformations of the amination products to useful skeletons.magnified image
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