Efficient synthesis of 2-arylquinazolines via copper-catalyzed dual oxidative benzylic CH aminations of methylarenes

A novel copper-catalyzed dual oxidative benzylic CH aminations of methylarenes with 2-aminobenzoketones in the presence of ammonium acetate was developed. This reaction represents a new avenue for 2-arylquinazolines with good yields. A key intermediate was detected and the kinetics isotope effect (KIE) indicated that CH bond cleavage was the rate-determining step.

A novel copper-catalyzed dual oxidative benzylic CH aminations of methylarenes with 2-aminobenzoketones in the presence of ammonium acetate was developed. This reaction represents a new avenue for 2-arylquinazolines with good yields.Figure optionsDownload as PowerPoint slide