Pd(II)-Catalyzed [3 + 1 + 1 + 1] Cascade Annulation of <i>N</i> -Substituted Anilines with CO and Amines: Direct Access to <i>N</i> 1, <i>N</i> 3-Disubstituted Quinazoline-2,4(1 <i>H</i> ,3 <i>H</i> )-diones

In this study, we present an efficient and direct strategy for the synthesis of N 1, N 3-disubstituted quinazoline-2,4(1 H,3 H )-diones with high atom and step economy. The protocol involves a Pd(II)-catalyzed [3 + 1 + 1 + 1] cascade carbonylation/amidation/cyclocarbonylation reaction, wherein the alkylamino moiety of simple N -substituted anilines serves as an intrinsic directing group, with CO and amines as the coupling partners. This cascade process proceeds smoothly with a variety of substrates under mild conditions, affording the target products with either identical or distinct substituents mostly in moderate to good yields.