Divergent synthesis of arylated pyridin-2 (1H)-one derivatives via metal-catalysed cross-coupling processes

JS Siddle, AS Batsanov, ST Caldwell, G Cooke…

Index: Siddle, Jamie S.; Batsanov, Andrei S.; Caldwell, Stuart T.; Cooke, Graeme; Bryce, Martin R. Tetrahedron, 2010 , vol. 66, # 32 p. 6138 - 6149

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Citation Number: 17

Abstract

1, 5-Di (hetero) arylated-pyridin-2 (1H)-one derivatives have been readily obtained in good yields starting from 2-fluoro-5-pyridylboronic acid. The sequence comprises three steps:(i) palladium-catalysed Suzuki-Miyaura reaction;(ii) base-catalysed hydrolysis;(iii) copper- catalysed C–N coupling. X-ray crystal structures are reported for selected pyridin-2 (1H)-one derivatives. These compounds are of interest as new scaffolds for drug discovery.