Synthesis of hindered biphenyls by sequential non-transition metal-catalyzed reaction/palladium-catalyzed cross-couplings

The sequential reaction of 1,2-dihalobenzenes with aryllithiums followed by palladium-catalyzed cross-coupling reactions with Grignard reagents and arylboronic acids is described. This sequential reaction provides a convenient and expeditious access to tri-ortho substituted biaryl derivatives.

Non-transition metal-catalyzed reactions of 1,2-dihalobenzene with aryllithiums followed by palladium-catalyzed cross-coupling reactions of Grignard reagents and arylboronic acids to form tri-ortho substituted biphenyls are described.