Copper‐Catalyzed Tandem C−H/N−H Activation, Cyclization[4+2] and Dehydration of Arylamides with Formamide: Synthesis of 4(3H)‐Quinazolinones Derivatives

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A novel route for copper‐catalyzed tandem C−H/N−H activation, cyclization[4+2] and dehydration of arylamides with formamide to synthesize 4(3H)‐quinazolinone derivatives was developed. This approach is assisted by an 8‐aminoquinoline group and the formamide provide the nitrogen and carbon source. This reaction is compatible with various functional groups, and the reaction conditions are mild. In addition, it uses cheaply and commercially available reagents, and provides direct access to 4(3H)‐quinazolinones.