This method shows effective asymmetric pyridonation of conjugated dienes, suggesting improved reactivity with a cocatalyst.
A novel palladium-catalyzed asymmetric aminomethylative pyridonation of conjugated dienes with N,O-acetals and 2-hydroxypyridines was established, which provided a direct and reliable method for the synthesis of a wide range of γ-aminated N-substituted 2-pyridones with good to excellent enantioselectivities. The simple BF3 was identified as an effective cocatalyst to improve the reaction efficiency, and DFT calculations revealed that proton transfer between the aminomethylated allylic palladium species and 2-hydroxypyridine promoted by BF3 is crucial for obtaining good reactivity.
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Yang et al. (2025) studied this question.
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