Lewis Base-Mediated [3 + 3] Cycloaddition of <i>N</i> -2,2,2-Trifluoroethylisatin Ketimines with Diazo Esters: Synthesis of Trifluoromethyl-1,2,4-triazine-spirooxindoles
A facile and efficient DBU-mediated [3 + 3] cycloaddition reaction of <i>N</i>-2,2,2-trifluoroethylisatin ketimines with diazo esters for the synthesis of trifluoromethyl dihydro-1,2,4-triazine-spirooxindole derivatives has been developed. The reaction proceeds under mild conditions with a broad substrate scope, tolerating various electronically and sterically diverse substituents to afford moderate to excellent yields. Furthermore, a one-pot cycloaddition/oxidation strategy is established to achieve efficient synthesis of trifluoromethyl-1,2,4-triazine-spirooxindoles. This study not only enriches the structural diversity of spirooxindoles but also provides a valuable synthetic tool for developing novel bioactive molecules in medicinal chemistry.
Authors
- Yuwei Zheng
- L Chen
- Lu Wang (ORCID: https://orcid.org/0000-0002-0073-0666)
- Yiran Wang
- Xiaopeng Qiu
- Yan Fu
- Jianmin Gu
- Fei Xu
- Ran Guo
- Wenhe Shi
- Ruijuan Xing
Institutions
- Hebei Medical University (CN)
- Center for Drug Evaluation and Research (US)
- Centerstone (US)
- Medicina (PL)
Publication Details
- Journal
- The Journal of Organic Chemistry
- Published
- 2026-03-13
- DOI
- https://doi.org/10.1021/acs.joc.5c03258
- Primary Topic
- Fluorine in Organic Chemistry
- Type
- article
- Field-Weighted Citation Impact
- 0.00