Direct C1–H Amination of Free NH Carbazoles Enabled by the Catellani Reaction

Abstract

Carbazoles are valuable building blocks for emerging pharmaceuticals and bioactive compounds. However, methods to access C1–H-aminated carbazoles remain underdeveloped. Current approaches often require multistep syntheses or the use of toxic metals. Herein, we report the first Pd/NBE-catalyzed C1–H amination of NH-free carbazoles. The method introduces a broad range of cyclic amines onto carbazole scaffold and tolerates several functional groups, including acyl, pivaloyl, and halogen substituents. This approach expands the scope of the Catellani reactions to the direct amination of unprotected carbazoles, offering a concise entry to otherwise challenging C1-aminated scaffolds.