Palladium-Catalyzed Late-Stage Alkenylation of Aryl Fluorosulfonates and Phenol-Containing Drugs

A modular palladium-catalyzed alkenylation of a number of aryl fluorosulfonates and phenol-containing drugs such as estrone, pterostilbene, 6-hydroxyflavone, and other phenol-based pharmaceuticals has been developed. This method enables economical and chemoselective alkenylation of aryl fluorosulfonates with <i>N</i>-tosylhydrazones even in the presence of chloro functionalities, achieving high yields and excellent functional group compatibility. The strategy demonstrates broad application potential in the fields of pharmaceutical and agricultural chemical synthesis.

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Publication Details

Journal
Organic Letters
Published
2026-03-22
DOI
https://doi.org/10.1021/acs.orglett.6c00522
Primary Topic
Catalytic C–H Functionalization Methods
Type
article
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article

Palladium-Catalyzed Late-Stage Alkenylation of Aryl Fluorosulfonates and Phenol-Containing Drugs

Xin‐Xing Wu, Mingxia Wu, Yanfang Shang, Haoyu Cheng et al.
Organic Letters
Catalytic C–H Functionalization Methods
article

Palladium-Catalyzed Late-Stage Alkenylation of Aryl Fluorosulfonates and Phenol-Containing Drugs

Xin‐Xing Wu, Mingxia Wu, Yanfang Shang, Haoyu Cheng, Yu Meng, Jingwen Xi
article en

Abstract

A modular palladium-catalyzed alkenylation of a number of aryl fluorosulfonates and phenol-containing drugs such as estrone, pterostilbene, 6-hydroxyflavone, and other phenol-based pharmaceuticals has been developed. This method enables economical and chemoselective alkenylation of aryl fluorosulfonates with <i>N</i>-tosylhydrazones even in the presence of chloro functionalities, achieving high yields and excellent functional group compatibility. The strategy demonstrates broad application potential in the fields of pharmaceutical and agricultural chemical synthesis.

Organic Letters
Nantong University (CN)
Zero hunger
Openalex Percentile: Top 12%
Catalytic C–H Functionalization Methods
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