The unprecedented Pd(II)-catalyzed cascade annulation of o-aminobenzoic acids with CO, amines, and aldehydes has been developed. This protocol provides an efficient and concise approach to selective construction of N3-substituted and N1,N3disubstituted 2,3-dihydroquinazolin-4(1H)-ones mostly in moderate to excellent yields from simple and easily available starting materials under mild conditions featured with low cost, high step economy, broad substrate scope, and good product diversity.
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