Pd-catalyzed ortho-C–H arylation of free anilines with arylboric acids forming o-amino biaryls

Abstract

We report a Pd-catalyzed ortho-C–H arylation of free anilines with arylboric acids. Under the reaction conditions, a wide range of arylboric acids can couple with free anilines to produce the corresponding o-amino biaryls in moderate to good yields with good functional group tolerance. This reaction can be conducted on the gram scale. The products can be easily further functionalized via transformation of the free amino group. These results indicate the potential synthetic value of this new reaction in organic synthesis.