Peer-reviewedCC BYRSC advances
Synthesis and diversification of SuFEx-active 2H-indazoles from azobenzenes and ethenesulfonyl fluoride.
5 affiliations
- 1College of Pharmacy, Korea University Sejong 30019 Republic of Korea [email protected].
- 2Institute of Pharmaceutical Science and Translational Research, Korea University Sejong 30019 Republic of Korea.
- 3Department of Innovative Pharmaceutical Sciences, Kyungpook National University Daegu 41566 Republic of Korea [email protected].
- 4College of Pharmacy, Research Institute of Pharmaceutical Sciences, Sookmyung Women's University Seoul 04310 Republic of Korea.
- 5Department of Chemistry, Sungkyunkwan University Suwon 16419 Republic of Korea [email protected].
Abstract
A direct approach to SuFEx-active 2H-indazoles from azobenzenes and ethenesulfonyl fluoride was developed through Rh(iii)-catalyzed tandem C-H activation and annulation. The transformation provided a range of SO₂F-containing 2H-indazoles with good functional group tolerance while preserving the synthetically valuable sulfonyl fluoride functionality. The practicality of the method was demonstrated by gram-scale synthesis and subsequent SuFEx conjugation with representative biologically relevant molecules. This strategy provides efficient access to functionalized 2H-indazoles bearing a versatile SuFEx handle for further molecular diversification in medicinal chemistry and chemical biology.
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BibTeX
@article{rajaka2026synthesis,
title = {{Synthesis and diversification of SuFEx-active 2H-indazoles from azobenzenes and ethenesulfonyl fluoride.}},
author = {Lingayya Rajaka and Hyosik Woo and Myunghwa Jung and Chanhee Jang and Seungwan Kim and Jihyo Lee and Saegun Kim and Sangil Han and Han Yong Bae and Sang Hoon Han},
journal = {RSC advances},
year = {2026},
month = oct,
doi = {10.1039/d6ra09632h},
url = {https://europepmc.org/article/MED/42898774},
note = {CC BY},
}
RIS
TY - JOUR
TI - Synthesis and diversification of SuFEx-active 2H-indazoles from azobenzenes and ethenesulfonyl fluoride.
AU - Lingayya Rajaka
AU - Hyosik Woo
AU - Myunghwa Jung
AU - Chanhee Jang
AU - Seungwan Kim
AU - Jihyo Lee
AU - Saegun Kim
AU - Sangil Han
AU - Han Yong Bae
AU - Sang Hoon Han
PY - 2026
DA - 2026/10/19
JO - RSC advances
DO - 10.1039/d6ra09632h
UR - https://europepmc.org/article/MED/42898774
AB - A direct approach to SuFEx-active 2H-indazoles from azobenzenes and ethenesulfonyl fluoride was developed through Rh(iii)-catalyzed tandem C-H activation and annulation. The transformation provided a range of SO₂F-containing 2H-indazoles with good functional group tolerance while preserving the synthetically valuable sulfonyl fluoride functionality. The practicality of the method was demonstrated by gram-scale synthesis and subsequent SuFEx conjugation with representative biologically relevant molecules. This strategy provides efficient access to functionalized 2H-indazoles bearing a versatile SuFEx handle for further molecular diversification in medicinal chemistry and chemical biology.
SN - 2046-2069
ER -