One-Pot, Three-Component Cascade Synthesis of 4-Amino Quinoline Derivatives from 2-Aminobenzonitriles, Aldehydes, and Active Methylene Compounds
Abstract
-mediated one-pot, three-component methodology has been developed for the direct synthesis of a diverse array of 4-aminoquinoline derivatives utilizing 2-aminobenzonitriles, aldehydes, and active methylene compounds. The reaction proceeds smoothly via a series of tandem reactions, including condensation followed by intramolecular cyclization and aromatization, to afford highly substituted 4-aminoquinolines in good to excellent yields (up to 88%) within 12-14 h. The protocol exhibits a broad substrate scope and excellent functional group tolerance. Notably, the strategy can also be applied for the construction of highly fused polycyclic frameworks through C-H activation and annulation and allows for the efficient synthesis of diacylated derivatives, highlighting its broad synthetic utility.
Fields of Study & Subjects
Catalytic C–H Functionalization Methods
Multicomponent Synthesis of Heterocycles
Synthesis of heterocyclic compounds
Publication details
- Journal / source
- The Journal of Organic Chemistry
- Publisher
- American Chemical Society (ACS)
- Volume
- 91
- Issue
- 6
- Pages
- 2353–2364
- Publication date
- 30 January 2026
- Language
- EN