CO 2 -Driven C(sp 2 )–H Lactamization to 2-Quinolinones
Abstract
2-Quinolinones are key scaffolds in pharmaceuticals, yet their synthesis under mild and sustainable conditions remains challenging. We report a transition-metal-free C(sp 2 )–H lactamization of azido-alkenes using CO 2 as a one-carbon source. The reaction proceeds under mild conditions with dimethyl phenylphosphonite, affording 2-quinolinones with excellent functional-group tolerance. The method enables 13 C-labeling with 99% incorporation, gram-scale synthesis, and downstream functionalizations, providing access to biologically relevant molecules. This strategy provides a versatile alternative to conventional and metal-catalyzed quinolinone syntheses.
Fields of Study & Subjects
Catalytic C–H Functionalization Methods
Carbon dioxide utilization in catalysis
Cyclopropane Reaction Mechanisms
Publication details
- Journal / source
- Organic Letters
- Publisher
- American Chemical Society (ACS)
- Volume
- 28
- Issue
- 9
- Pages
- 3008–3011
- Publication date
- 23 February 2026
- Language
- EN