ol6b01762_si_003.cif (36.22 kB)

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

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posted on 15.07.2016, 15:05 by Wataru Miura, Koji Hirano, Masahiro Miura
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.