Synthesis of (Hetero)aryl Fused 4 <i>H</i> -Quinolizin-4-ones from <i>N</i> -Ts Substituted (Hetero)arylamides and Pyridotriazoles
This paper describes a practical synthetic method of (hetero)aryl fused 4<i>H</i>-quinolizin-4-ones via (hetero)aryl sp<sup>2</sup> C-H carbenoid functionalization of (hetero)aryl amides using pyridotriazoles with good functional group tolerance. This process demonstrates excellent site-selectivity, enabling the C-H functionalization reaction directed by an amide group by overcoming the interference of strong coordination between <i>N</i>-heterocycles and metal catalysis. The synthetic method represents an efficient strategy with attractive application prospects, including late-stage modification of drug molecules, total synthesis of natural products, and live-cell imaging.
Authors
- Yi Dong (ORCID: https://orcid.org/0000-0001-7844-7206)
- Hua Tian (ORCID: https://orcid.org/0000-0002-2316-1953)
- Xiao-Qiao Hong
- Heng Xu (ORCID: https://orcid.org/0000-0002-1720-5286)
- Bo Mei (ORCID: https://orcid.org/0000-0002-7114-7793)
- Yiting Chang (ORCID: https://orcid.org/0000-0001-5408-3292)
- Xin Yang (ORCID: https://orcid.org/0009-0000-9693-1325)
Institutions
- Guiyang Medical University (CN)
- Chinese Academy of Sciences (CN)
- Chinese Academy of Medical Sciences & Peking Union Medical College (CN)
- Peking Union Medical College Hospital (CN)
- Shanghai Institute of Materia Medica (CN)
- Institute of Medicinal Plant Development (CN)
Publication Details
- Journal
- Organic Letters
- Published
- 2025-12-09
- DOI
- https://doi.org/10.1021/acs.orglett.5c04190
- Primary Topic
- Catalytic C–H Functionalization Methods
- Type
- article
- Field-Weighted Citation Impact
- 0.00