Nickel( II ) Assisted One‐Pot Synthesis of Quinazolinones From Alcohols

ABSTRACT An efficient, eco‐friendly one‐pot synthesis of 2‐aryl quinazolinone derivatives through the dehydrogenative coupling of alcohols and 2‐aminobenzonitriles in the presence of a Ni(II) catalyst. The catalytic protocol was eco‐friendly, straightforward and provided the desired quinazolinone products with moderate to excellent yields (12 examples, yields ≤ 91%). The catalytic reaction was operated in low catalyst loading (5 mol%) water and hydrogen gas are the only by‐products. The control experiments and mechanistic studies confirm that the reaction proceeds via an aldehyde and cyclic aminol intermediate. Additionally, large‐scale synthesis of 2‐(p‐tolyl)quinazolin‐4(3H)‐one (72%) demonstrates the robustness of the present method.