Alkylation of Pyridone Derivatives By Nickel/Lewis Acid Catalysis


  • This work has been supported financially by MEXT in the form of a Grant-in-Aid for Scientific Research on Innovative Areas “Molecular Activation Directed toward Straightforward Synthesis” (to Y.N., No. 22105003), and JSPS in the form of the award Scientific Research (S) (to T.H., No. 21225005).


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MAD as an additive: The [Ni(cod)2], (2,6-tBu2-4-MeC6H2O)2AlMe (MAD), and N-heterocyclic carbene (NHC) catalytic system effected a highly regioselective alkylation of pyridone derivatives (see scheme). Substituted pyridones and related heterocycles react with both terminal and internal alkenes to selectively give a range of nitrogen-containing heterocycles with linear alkyl substituents.