Rhodium-Catalyzed C6-Selective C–H Borylation of 2-Pyridones

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• 作者：Wataru Miura ; Koji Hirano ; Masahiro Miura
• 刊名：Organic Letters
• 出版年：2016
• 出版时间：August 5, 2016
• 年：2016
• 卷：18
• 期：15
• 页码：3742-3745
• 全文大小：376K
• 年卷期：0
• ISSN：1523-7052

文摘

A pyridine-directed, rhodium-catalyzed C6-selective C–H borylation of 2-pyridones with bis(pinacolato)diboron (pinB–Bpin) has been developed. The reaction proceeds smoothly under relatively mild conditions, and the corresponding C6-borylated 2-pyridones are obtained with perfect site selectivity. Subsequent palladium-catalyzed Suzuki–Miyaura cross-coupling is followed by the removal of the pyridine directing group to form the C6-arylated NH-pyridone in an acceptable overall yield.