Citation: Tonghao Zhu, Chuxun Wu, Xiaoying Zhang, Zaixing Yang, Ning Mu, Wei Zhou, Jie Wu. Generation of 2,2-difluoro-4-sulfonylthiochromanes under visible light irradiation and their biological evaluations[J]. Chinese Chemical Letters, ;2026, 37(12): 112468. doi: 10.1016/j.cclet.2026.112468 shu

Generation of 2,2-difluoro-4-sulfonylthiochromanes under visible light irradiation and their biological evaluations

Tonghao Zhu ^{a, 1} ,
Chuxun Wu ^{b, 1} ,
Xiaoying Zhang ^a ,
Zaixing Yang ^a ,
Ning Mu ^{a, *,} ,
Wei Zhou ^{b, *,} ,
Jie Wu ^{a, c, d, *,}

a.
Taizhou First People's Hospital (Taizhou University affiliated First People's Hospital) & School of Pharmaceutical and Chemical Engineering, Taizhou University, Taizhou 318000, China
b.
Shanghai Medical College & Department of Chemistry, Fudan University, Shanghai 200438, China
c.
Key Laboratory of Organofluorine Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China
d.
School of Medicine, Hangzhou City University, Hangzhou 310015, China

mnwsp@163.com

zhouw@fudan.edu.cn

jie_wu@fudan.edu.cn

Received Date: 26 October 2025
Revised Date: 16 January 2026
Accepted Date: 27 January 2026
Available Online: 29 January 2026

Figures(6)

A facile route to 2,2-difluoro-4-sulfonylthiochromanes through a reaction of {difluoro(phenylthio)methyl}triphenylphosphonium iodides with vinyl sulfones under visible light irradiation is reported. This transformation is highly efficient through radical difluoro(phenylthio)methylation/cyclization in the absence of catalyst and additives under mild conditions. The structure of 2,2-difluoro-4-(phenylsulfonyl)thiochromanes is found to be a novel structure for anti-influenza, and further structure-activity relationship (SAR) studies show that cyano and fluoro substitution on phenyl and thiochromanes, respectively, can improve the activity significantly. The supposed mechanism of hemagglutinin inhibition is also investigated by molecular docking analysis.
- Anti-influenza,
- Vinyl sulfone,
- {Difluoro(phenylthio)methyl}triphenylphosphonium iodide,
- 2,2-Difluoro-4-sulfonylthiochromane,
- Visible light irradiation
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