Pd(II)-Catalyzed [3 + 1 + 1 + 1] Cascade Annulation of N -Substituted Anilines with CO and Amines: Direct Access to N 1, N 3-Disubstituted Quinazoline-2,4(1 H ,3 H )-diones
Abstract
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.
Fields of Study & Subjects
Quinazolinone synthesis and applications
Carbon dioxide utilization in catalysis
Catalytic C–H Functionalization Methods
Publication details
- Journal / source
- Organic Letters
- Publisher
- American Chemical Society (ACS)
- Volume
- 28
- Issue
- 13
- Pages
- 3947–3954
- Publication date
- 16 February 2026
- Language
- EN