Syntheses of 4-(Heteroaryl)cyclohexanones via Palladium-Catalyzed Ester α-Arylation and Decarboxylation.

ABSTRACT

An alternative synthesis of 4-(heteroaryl)cyclohexanones is described featuring a palladium-catalyzed ester α-arylation followed by decarboxylation. The substrate scope is broad with a wide range of heteroaryl halides. In particular, the reaction robustness is demonstrated by the synthesis of >10 g of 4-(pyrazin-2-yl)cyclohexanone with 85% overall yield.