Rh(III)‐Catalyzed Selective ortho‐C−H Amination of Benzoic Acids with Anthranils: A Facile Access to Anthranilic Acid Derivatives (AAs)

Abstract An efficient Rh(III)‐catalyzed Csp 2 ‐H amination protocol of benzoic acids with anthranils was developed for the rapid assembly of valuable anthranilic acid derivatives (AAs). The weakly coordinating carboxyl acted as a directing group and was further transformed to an ester group after facilitating the first C−H amination process. This reaction features good functional group tolerance, mild conditions and operational simplicity. The synthetic potential of this methodology was demonstrated by the synthesis of various useful heterocycles and derivatives.