Synthesis and diversification of SuFEx-active 2H-indazoles from azobenzenes and ethenesulfonyl fluoride.

Authors

Lingayya Rajaka, Hyosik Woo, Myunghwa Jung, Chanhee Jang, Seungwan Kim, Jihyo Lee, Saegun Kim, Sangil Han, Han Yong Bae, Sang Hoon Han

Published in

RSC advances. Oct 19, 2026. Epub Oct 19, 2026.

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.

PMID:
42898774
Bibliographic data and abstract were imported from PubMed on 20 Oct 2026.

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