Monoprotected l‐Amino Acid (l‐MPAA), Accelerated Bromination, Chlorination, and Iodination of C(sp2)−H Bonds by Iridium(III) Catalysis

Abstract Halogenated arenes are important structural motifs commonly found in biologically active molecules and used for a variety of transformations in organic synthesis. Herein, we report the mono‐protected l ‐amino acid ( l ‐MPAA) accelerated iridium(III)‐catalyzed halogenation of (hetero)anilides at room temperature. This reaction constitutes the first example of an iridium(III)/ l ‐MPAA‐catalyzed general halogenation of (hetero)arenes through C(sp 2 )−H activation. Furthermore, we demonstrate the potential utility of our method through its use in the synthesis of a quinolone derivative.