Cu‐Mediated Amination of (Hetero)Aryl C−H bonds with NH Azaheterocycles

Direct synthesis of N‐(hetero)arylated heteroarenes has been realized through Cu‐mediated C−N coupling of NH azaheterocycles with aryl C−H bonds under aerobic conditions. This method features a broad scope of both heterocyclic arenes (pyridine, quinoline, pyrazole, imidazole, furan, thiophene, benzofuran, and indole) and NH azaheterocycles (imidazole, pyrazole, indole, azindole, purine, indazole, benzimidazole, pyridone, carbazole), providing a versatile method for the synthesis of pharmaceutically important N‐(hetero)arylated heteroarenes. The versatility of this reaction was further demonstrated through late‐stage modification of marketed drugs and the synthesis of a key intermediate for accessing a class of angiotensin II receptor 1 antagonists.