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

A convenient C−H amination of quinoxalin‐2‐ones has been developed. This transformation provides concise access to 3‐aminoquinoxalin‐2(1H)‐ones with a broad tolerance of functional groups, utilizing TMSN3 as an amino source under simple and mild conditions. The target 3‐aminoquinoxalin‐2(1H)‐ones are important intermediates for the synthesis of biologically active 3‐N‐substituted quinoxalin‐2‐one derivatives.