Copper‐Catalyzed Intramolecular C─H Amidation of N,N′‐Disubstituted Ureas for the Synthesis of Benzimidazol‐2‐ones

Abstract

A novel methodology has been reported for the synthesis of benzimidazol‐2‐ones via copper‐catalyzed direct intramolecular C─H amidation of N,N′‐disubstituted ureas. This method exhibits a broad substrate scope and good functional‐group tolerance, providing a wide range of benzimidazol‐2‐ones in good to high yields. Furthermore, to the best of our knowledge, this is the first method that enables the conversion of challenging ureas bearing primary aliphatic amines into benzimidazol‐2‐ones. The synthetic potential of present method is further demonstrated through gram‐scale reactions and derivatization studies.