Spirocyclization-Enabled Remote Phosphorothiolation of Nonactivated Arenes via Dual Photoredox/Copper-Catalyzed Dearomatization

Spirocyclic frameworks are key structural motifs in bioactive molecules, driving ongoing efforts to develop efficient and sustainable synthetic methods. Herein, we report a synergistic photocatalysis/copper dual-catalytic system that enables direct dearomative spirocyclization via the simultaneous incorporation of phosphorothioate groups in a single synthetic operation. This strategy allows rapid, selective construction of complex spirocenters from simple nonactivated aromatic precursors, exhibits broad substrate scope, including bioactive relevant scaffolds, and provides a robust platform for diversity-oriented synthesis with significant potential in drug discovery.

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Publication Details

Journal
Organic Letters
Published
2026-04-06
DOI
https://doi.org/10.1021/acs.orglett.6c00996
Primary Topic
Sulfur-Based Synthesis Techniques
Type
article
Field-Weighted Citation Impact
0.00

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article

Spirocyclization-Enabled Remote Phosphorothiolation of Nonactivated Arenes via Dual Photoredox/Copper-Catalyzed Dearomatization

Yuzhen Gao, Weiping Su, Yu Du, Jiale Zhang et al.
Organic Letters
Sulfur-Based Synthesis Techniques
article

Spirocyclization-Enabled Remote Phosphorothiolation of Nonactivated Arenes via Dual Photoredox/Copper-Catalyzed Dearomatization

Yuzhen Gao, Weiping Su, Yu Du, Jiale Zhang, Siqing Liu, Denghui Ma
article en

Abstract

Spirocyclic frameworks are key structural motifs in bioactive molecules, driving ongoing efforts to develop efficient and sustainable synthetic methods. Herein, we report a synergistic photocatalysis/copper dual-catalytic system that enables direct dearomative spirocyclization via the simultaneous incorporation of phosphorothioate groups in a single synthetic operation. This strategy allows rapid, selective construction of complex spirocenters from simple nonactivated aromatic precursors, exhibits broad substrate scope, including bioactive relevant scaffolds, and provides a robust platform for diversity-oriented synthesis with significant potential in drug discovery.

Organic LettersVol. 28(15)
Ningbo University of Technology (CN), Fujian Institute of Research on the Structure of Matter (CN), University of Chinese Academy of Sciences (CN), Fuzhou University (CN)
National Natural Science Foundation of China, Haixi Institute, Chinese Academy of Sciences, Natural Science Foundation of Fujian Province, Ningbo University of Technology, National Key Research and Development Program of China, Fujian Science and Technology Innovation Laboratory for Optoelectronic Information of China
Responsible consumption and production
Openalex Percentile: Top 23%
Sulfur-Based Synthesis Techniques
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