# Carbamothioate-mediated Selectfluor™ oxidation for the synthesis of benzenesulfonyl fluorides in chalcone derivatives

**Authors:** Boye Jiang, Juan Zhang, Boning Wang, Airui Zhou, Yan Zou, Qingguo Meng, Qingjie Zhao, Xiaoyun Chai, Conghao Gai

PMC · DOI: 10.1039/d5ra03427b · RSC Advances · 2025-06-27

## TL;DR

A new method for making benzenesulfonyl fluorides from chalcone derivatives avoids unwanted side reactions and is useful for drug discovery.

## Contribution

A novel carbamothioate-mediated oxidation method for synthesizing sulfonyl fluorides in chalcone derivatives is introduced.

## Key findings

- The method avoids Michael addition side reactions in chalcone derivatives.
- It provides moderate yields and good functional group tolerance.
- The approach is applicable to covalent drug discovery by incorporating sulfonyl fluoride warheads.

## Abstract

A carbamothioate-mediated method for synthesizing benzenesulfonyl fluorides via Selectfluor™ oxidation is reported, enabling compatibility with α,β-unsaturated chalcone derivatives without Michael addition side reactions. This approach offers moderate yields, broad functional group tolerance, and applications in covalent drug discovery, facilitating the incorporation of sulfonyl fluoride warheads into complex electrophilic scaffolds.

Novel carbamothioate-mediated sulfonyl fluoride synthesis enables chalcone functionalization without Michael addition side reactions.

## Linked entities

- **Chemicals:** Carbamothioate (PubChem CID 2817513), Selectfluor™ (PubChem CID 2724933)

## Full-text entities

- **Chemicals:** Selectfluor (MESH:C408750), sulfonyl fluoride (MESH:C048899), chalcone (MESH:D002599), Carbamothioate (-)

## Full text

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## Figures

6 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12203147/full.md

## References

12 references — full list in the complete paper: https://tomesphere.com/paper/PMC12203147/full.md

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Source: https://tomesphere.com/paper/PMC12203147