Annulation of α-Diazo Sulfonium Salts with α-Vinylanilines via a Dicationic Intermediate toward Quinolines
α-Diazo sulfonium salts constitute a unique subclass of diazo reagents that integrate diazo and sulfonium functionalities within a single molecular scaffold. While their reactivity via carbene, radical, or carbyne intermediates has been extensively investigated, the synthetic utility of their proton-activated dicationic species remains largely unexplored. Herein, we report a Brønsted acid-promoted, metal-free annulation of α-diazo sulfonium salts with binucleophilic α-vinylanilines. This transformation proceeds through a protonation-induced polarity inversion at the diazo carbon, generating a dicationic intermediate bearing two electrophilic centers. Sequential intramolecular nucleophilic substitution of this intermediate enables efficient access to mono-, di-, and trisubstituted quinolines under mild conditions. This study showcases a rare example of dielectrophilic activation in diazo chemistry and establishes a complementary strategy for constructing heterocycles beyond conventional carbene-based pathways.
Authors
- Shuai Gao (ORCID: https://orcid.org/0000-0003-4630-7641)
- Qiang‐Qiang Li (ORCID: https://orcid.org/0000-0002-8268-7488)
- Ziqiang Zhang (ORCID: https://orcid.org/0000-0003-3808-162X)
- Bao‐Gui Cai (ORCID: https://orcid.org/0009-0009-2638-6275)
- Jun Xuan (ORCID: https://orcid.org/0000-0003-0578-9330)
- Xing Li (ORCID: https://orcid.org/0000-0001-9145-4769)
Institutions
- Ministry of Education of the People's Republic of China (CN)
- Anhui University (CN)
- Ministry of Education (BD)
Publication Details
- Journal
- Organic Letters
- Published
- 2025-08-11
- DOI
- https://doi.org/10.1021/acs.orglett.5c02541
- Citations
- 3
- Primary Topic
- Cyclopropane Reaction Mechanisms
- Type
- article
- Field-Weighted Citation Impact
- 2.81
Funders
- National Natural Science Foundation of China
- Natural Science Foundation of Anhui Province
- Excellent Young Talents Fund Program of Higher Education Institutions of Anhui Province