Advances in sulfur–fluoride exchange for chemical biology

09 December 2024, Version 1
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

Since their introduction as a new strategy for synthesizing diverse chemotypes, sulfur(VI)–fluoride exchange (SuFEx) transformations have found applications ranging from polymer chemistry and covalent probe development to bioconjugation tools and chemistries for the synthesis of compound libraries. The collection of SuFEx reactions has expanded significantly since their introduction as a concept, comprising functionalities with varying reactivities towards different nucleophiles; thus, enabling the generation of a wide array of sulfur-containing functional groups for the linkage of structural elements in diverse chemotypes. In this review, we focus on the most recent developments in the use of SuFEx chemistry as a means for the preparation of compound libraries for biological screening as well as the introduction of SuFEx hubs into various biomolecules.

Keywords

covalent inhibitors
latent electrophile
compound libraries
peptides
SuFEx

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