DBU-Mediated [3+3] Annulation of Indolin-3/2-ones and Ethenesulfonyl Fluorides: An Approach to Indole-Fused δ-Sultones
A general and efficient approach to the synthesis of various indole-fused δ-sultones has been developed via DBU-mediated [3+3] cyclizations of indolin-3/2-ones and β-(hetero)arylethenesulfonyl fluorides. Notably, the reaction shows a broad substrate scope, and over 70 examples were exhibited in up to 99% isolated yield. In addition, some of the synthesized compounds showed significant antitumor activity against HepG2 and Caco-2 cells <i>in vitro</i>, which might provide promising insights for the future discovery and rational design of novel antitumor agents.
Authors
- Meiling Tang (ORCID: https://orcid.org/0000-0002-2373-6083)
- Jun Xie (ORCID: https://orcid.org/0000-0003-1062-1102)
- Jianghong Li (ORCID: https://orcid.org/0000-0001-6487-8486)
- Yujiao He
- Zhuo‐Zhuo Zhang
- Wei Huang (ORCID: https://orcid.org/0000-0003-0832-1864)
- Ting Peng (ORCID: https://orcid.org/0000-0003-1458-1603)
- Lin Chen (ORCID: https://orcid.org/0000-0002-9270-1626)
- Jun‐Long Li (ORCID: https://orcid.org/0000-0002-4700-0142)
Institutions
- Chengdu University (CN)
- Chengdu University of Traditional Chinese Medicine (CN)
Publication Details
- Journal
- The Journal of Organic Chemistry
- Published
- 2025-04-09
- DOI
- https://doi.org/10.1021/acs.joc.5c00088
- Citations
- 2
- Primary Topic
- Organic and Inorganic Chemical Reactions
- Type
- article
- Field-Weighted Citation Impact
- 1.51
Funders
- National Natural Science Foundation of China
- Department of Science and Technology of Sichuan Province
- Special Project for Research and Development in Key areas of Guangdong Province