Divergent Synthesis of Multisubstituted Hydroindole Derivatives via [3+2] Annulations of <i>p</i>‐Quinamines with Nitroalkenes
Abstract The synthesis of two stereoisomers of hydroindole derivatives was achieved through [3+2] annulations of p ‐quinamines with nitroalkenes. Catalyst‐free or in the presence of DMAP, the annulation reactions were employed to produce the target products containing four contiguous stereogenic centers. This method enables the efficient construction of multisubstituted and functionalized hydroindole derivatives from readily accessible building blocks and reagents. Furthermore, the anti‐inflammatory activity of some resulting hydroindoles was evaluated, with three derivative products showing effective inhibition of NLRP3 inflammasome activation.
Authors
- Yan Ding (ORCID: https://orcid.org/0000-0003-3119-9529)
- Zengwei Lai (ORCID: https://orcid.org/0000-0001-7684-1154)
- Baoluo Wan (ORCID: https://orcid.org/0000-0002-4889-1370)
- Yi Huang (ORCID: https://orcid.org/0000-0003-0456-3428)
- Didi Liu (ORCID: https://orcid.org/0000-0002-4248-0669)
- Liang‐Hua Zou (ORCID: https://orcid.org/0000-0003-0939-6016)
- Hao Qin (ORCID: https://orcid.org/0000-0001-8137-2524)
- Zhe Liu (ORCID: https://orcid.org/0000-0001-5796-4335)
- Haonan Zong
Institutions
- Jiangnan University (CN)
Publication Details
- Journal
- Advanced Synthesis & Catalysis
- Published
- 2024-08-26
- DOI
- https://doi.org/10.1002/adsc.202400647
- Citations
- 3
- Primary Topic
- Synthesis and Characterization of Pyrroles
- Type
- article
- Field-Weighted Citation Impact
- 0.75
Funders
- National Natural Science Foundation of China
- Natural Science Foundation of Jiangsu Province