4.7 Article

Manganese-Mediated C3-Selective Direct Alkylation and Arylation of 2-Pyridones with Diethyl Malonates and Arylboronic Acids

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JOURNAL OF ORGANIC CHEMISTRY
卷 79, 期 3, 页码 1377-1385

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AMER CHEMICAL SOC
DOI: 10.1021/jo4027885

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  1. MEXT, Japan
  2. JSPS, Japan
  3. Grants-in-Aid for Scientific Research [25620084] Funding Source: KAKEN

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A manganese-mediated dehydrogenative direct alkylation of 2-pyridones with diethyl malonates has been developed. A similar reaction system is applicable to the direct arylation with arylboronic acids. These manganese-based reactions occur regioselectively at the C3 position of the 2-pyridones. The observed high C3 regioselectivity can complement precedented C-H functionalization protocols of the 2-pyridones in view of the site selectivity.

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