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.

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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

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article

Annulation of α-Diazo Sulfonium Salts with α-Vinylanilines via a Dicationic Intermediate toward Quinolines

Shuai Gao, Qiang‐Qiang Li, Ziqiang Zhang, Bao‐Gui Cai et al.
3 citations
Organic Letters
Cyclopropane Reaction Mechanisms
2.81
article

Annulation of α-Diazo Sulfonium Salts with α-Vinylanilines via a Dicationic Intermediate toward Quinolines

Shuai Gao, Qiang‐Qiang Li, Ziqiang Zhang, Bao‐Gui Cai, Jun Xuan, Xing Li
article en
3 citations

Abstract

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.

Organic LettersVol. 27(33)
Ministry of Education of the People's Republic of China (CN), Anhui University (CN), Ministry of Education (BD)
National Natural Science Foundation of China, Natural Science Foundation of Anhui Province, Excellent Young Talents Fund Program of Higher Education Institutions of Anhui Province
Openalex Percentile: Top 10%
Cyclopropane Reaction Mechanisms
2.81
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