Photocatalytic [4 + 1] Cycloaddition Access to Multisubstituted 2-Imino-2,5-dihydrofurans
Isocyanide radical cyclization, typically restricted to aryl isocyanides, is hampered by complex radical precursors. We've developed a strategy that overcomes this constraint by integrating [4 + 1] cyclization with a multifunctional system, which extends to alkyl and biomolecule-derived isocyanides and achieves a rare 1,2,3,4-tetrasubstitution of <i>α,β</i>-unsaturated carbonyls. Over 50 2-imino-2,5-dihydrofuran derivatives have been synthesized, allowing for molecular skeleton editing into valuable frameworks. These derivatives show antitumor activity, indicating their potential in drug development.
Authors
- Peng‐Ju Xia (ORCID: https://orcid.org/0000-0002-6587-3465)
- Zhipeng Ye (ORCID: https://orcid.org/0000-0002-3384-2779)
- Danna Chen (ORCID: https://orcid.org/0000-0002-8179-7888)
- Li-Ning Chen
- Shanshan Li (ORCID: https://orcid.org/0000-0001-6443-958X)
- Zhen Hong (ORCID: https://orcid.org/0000-0002-0014-6873)
- Juan Luo (ORCID: https://orcid.org/0000-0003-3775-9187)
- Cheng‐Xue Pan (ORCID: https://orcid.org/0000-0003-3437-2462)
Institutions
- Ministry of Education of the People's Republic of China (CN)
- Hainan Normal University (CN)
- Guangxi Normal University (CN)
Publication Details
- Journal
- Organic Letters
- Published
- 2025-09-01
- DOI
- https://doi.org/10.1021/acs.orglett.5c03227
- Citations
- 2
- Primary Topic
- Catalytic C–H Functionalization Methods
- Type
- article
- Field-Weighted Citation Impact
- 1.87
Funders
- National Natural Science Foundation of China
- Guangxi Normal University
- Science and Technology Department of Guangxi Zhuang Autonomous
- People's Government of Guangxi Zhuang Autonomous Region