Pd(II)-Catalyzed Cascade Annulation of o-Aminobenzoic Acids with CO, Amines, and Aldehydes to N3-/N1,N3-Substituted 2,3-Dihydroquinazolin-4(1H)-ones

The unprecedented Pd(II)-catalyzed cascade annulationof o-aminobenzoic acids with CO, amines, and aldehydeshasbeen developed. This protocol provides an efficient and concise approachto selective construction of N3-substituted and N1,N3-disubstituted 2,3-dihydroquinazolin-4(1H)-ones mostly in moderate to excellent yields from simpleand easily available starting materials under mild conditions featuredwith low cost, high step economy, broad substrate scope, and goodproduct diversity.

Automated summary

An unprecedented Pd(II)-catalyzed cascade annulation of o-aminobenzoic acids with CO, amines, and aldehydes has been developed. This method provides an efficient and concise approach for the selective construction of N3-substituted and N1,N3-disubstituted 2,3-dihydroquinazolin-4(1H)-ones, mostly in moderate to excellent yields, from simple and easily available starting materials under mild conditions characterized by low cost, high step economy, broad substrate scope, and good product diversity.