Department of Applied Chemistry, Faculty of Engineering, Osaka University , Suita, Osaka 565-0871, Japan.
J Org Chem. 2014 Feb 7;79(3):1377-85. doi: 10.1021/jo4027885. Epub 2014 Jan 29.
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.
发展了一种锰介导的 2-吡啶酮与丙二酸二乙酯的脱氢直接烷基化反应。类似的反应体系可适用于与硼酸芳基的直接芳基化反应。这些基于锰的反应在 2-吡啶酮的 C3 位发生区域选择性。鉴于反应的位点选择性,观察到的高 C3 区域选择性可以补充 2-吡啶酮的先前 C-H 官能化反应方案。