DTBP mediated tandem oxidative reaction of <i>o</i>-aminobenzamides with alcohols for the synthesis of quinazolinones

A practical and efficient methodology for the construction of quinazolinones from readily available alcohols and <i>o</i>-aminobenzamides in the presence of DTBP/Cu(OTf)₂ has been developed. This catalytic system exhibits good functional group tolerance and could afford a range of quinazolinones in good to excellent yields. In case of gram-scale reaction, 2-phenylquinazolin-4(3<i>H</i>)-one (<b>3a</b>) was obtained in 86% isolated yield, which indicated this protocol was amenable to scale up and had a potential value in industry. In addition, a plausible reaction mechanism involving a radical process has been proposed, and further applications of this catalytic system are under way in our laboratory.