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Peer-reviewedCC BYACS central science

Late-Stage Radical (Radio)fluorosulfonylation of Amines with [19F]fluoride and [18F]fluoride

  • Juanjuan Wang1
  • Yiwei Huang2
  • Zhiwei Xiao2
  • Yong He2
  • Yongkang Gai3,4
  • Dan Xu2
  • Kui Xu2
  • Zhiqing Su5
  • Xiao Shen6
  • Qiang Cheng1,7
7 affiliations
  1. 1Hubei Research Center of Fundamental Science-Chemistry, Engineering Research Center of Organosilicon Compounds and Materials, Ministry of Education, College of Chemistry and Molecular Sciences, Wuhan University, Wuhan 430072, China
  2. 2Department of Nuclear Medicine, Zhongnan Hospital of Wuhan University, Wuhan 430071, China
  3. 3Department of Nuclear Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430022, China
  4. 4Hubei Province Key Laboratory of Molecular Imaging, Wuhan 430022, China
  5. 5Wuhan HTA Pharmaceutical Company Ltd., Wuhan 430075, China
  6. 6The Institute for Advanced Studies, Wuhan University, Wuhan 430072, China
  7. 7Taikang Center for Life and Medical Sciences, Wuhan University, Wuhan 430072, China
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Abstract

Late-stage labeling with fluorine-18 serves to advance clinical care and drug discovery via positron emission tomography (PET). This goal motivates efforts to expand the accessible chemical space with tailored 18F-containing groups. Sulfamoyl fluorides are promising because of their potential physiological stability. Existing synthetic routes largely depend on group-transfer protocols from preformed fluorosulfonyl reagents. As a result, synthetic methods for [18F]­sulfamoyl fluorides are fundamentally based on isotope exchange. None of the methods have enabled a no-carrier-added (NCA) protocol for radiofluorosulfonylation of amines. Herein, we provide nitrogen-centered radical-mediated assembling fluorosulfonylation reactions, enabling conversion of abundant NH-containing substrates into sulfamoyl fluorides with [19F]­fluoride and [18F]­fluoride as an exclusive fluorine source. Our method features high functional group tolerance, broad NH-substrates, and an NCA radiochemical technique. The initial preclinical evaluation of the freshly synthesized [18F]­SUFA-flurpiridaz and its in vivo myocardial perfusion PET imaging collectively highlights the potential physiological stability of sulfamoyl [18F]­fluoride groups and the potential application of our radical radiofluorosulfonylation strategy.

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Cite

BibTeXRIS
BibTeX
@article{wang2026latestage,
  title = {{Late-Stage Radical (Radio)fluorosulfonylation of Amines with [19F]fluoride and [18F]fluoride}},
  author = {Juanjuan Wang and Yiwei Huang and Zhiwei Xiao and Yong He and Yongkang Gai and Dan Xu and Kui Xu and Zhiqing Su and Xiao Shen and Qiang Cheng},
  journal = {ACS central science},
  year = {2026},
  month = sep,
  doi = {10.1021/acscentsci.6c00992},
  url = {https://europepmc.org/article/PMC/PMC13720925},
  note = {CC BY},
}
RIS
TY  - JOUR
TI  - Late-Stage Radical (Radio)fluorosulfonylation of Amines with [19F]fluoride and [18F]fluoride
AU  - Juanjuan Wang
AU  - Yiwei Huang
AU  - Zhiwei Xiao
AU  - Yong He
AU  - Yongkang Gai
AU  - Dan Xu
AU  - Kui Xu
AU  - Zhiqing Su
AU  - Xiao Shen
AU  - Qiang Cheng
PY  - 2026
DA  - 2026/09/17
JO  - ACS central science
DO  - 10.1021/acscentsci.6c00992
UR  - https://europepmc.org/article/PMC/PMC13720925
AB  - Late-stage labeling with fluorine-18 serves to advance clinical care and drug discovery via positron emission tomography (PET). This goal motivates efforts to expand the accessible chemical space with tailored 18F-containing groups. Sulfamoyl fluorides are promising because of their potential physiological stability. Existing synthetic routes largely depend on group-transfer protocols from preformed fluorosulfonyl reagents. As a result, synthetic methods for [18F]­sulfamoyl fluorides are fundamentally based on isotope exchange. None of the methods have enabled a no-carrier-added (NCA) protocol for radiofluorosulfonylation of amines. Herein, we provide nitrogen-centered radical-mediated assembling fluorosulfonylation reactions, enabling conversion of abundant NH-containing substrates into sulfamoyl fluorides with [19F]­fluoride and [18F]­fluoride as an exclusive fluorine source. Our method features high functional group tolerance, broad NH-substrates, and an NCA radiochemical technique. The initial preclinical evaluation of the freshly synthesized [18F]­SUFA-flurpiridaz and its in vivo myocardial perfusion PET imaging collectively highlights the potential physiological stability of sulfamoyl [18F]­fluoride groups and the potential application of our radical radiofluorosulfonylation strategy.
SN  - 2374-7943
SN  - 2374-7951
ER  -