Direct C(sp2)−H Amination to Synthesize Primary 3‐aminoquinoxalin‐2(1H)‐ones under Simple and Mild Conditions

Abstract A convenient C−H amination of quinoxalin‐2‐ones has been developed. This transformation provides concise access to 3‐aminoquinoxalin‐2(1 H )‐ones with a broad tolerance of functional groups, utilizing TMSN 3 as an amino source under simple and mild conditions. The target 3‐aminoquinoxalin‐2(1 H )‐ones are important intermediates for the synthesis of biologically active 3‐ N ‐substituted quinoxalin‐2‐one derivatives. magnified image