CO <sub>2</sub> -Driven C(sp <sup>2</sup> )–H Lactamization to 2-Quinolinones
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<sup>2</sup>)-H lactamization of azido-alkenes using CO<sub>2</sub> 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 <sup>13</sup>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.
Authors
- Duanyang Kong (ORCID: https://orcid.org/0000-0002-1856-6323)
- Hong Sun
Institutions
- Kementerian Pendidikan Malaysia (MY)
- Beijing University of Chemical Technology (CN)
Publication Details
- Journal
- Organic Letters
- Published
- 2026-02-23
- DOI
- https://doi.org/10.1021/acs.orglett.6c00254
- Primary Topic
- Catalytic C–H Functionalization Methods
- Type
- article
- Field-Weighted Citation Impact
- 0.00