ChemistryEurope, Год журнала: 2025, Номер unknown

Опубликована: Апрель 13, 2025

Chemical modification of biomolecules such as peptides and proteins is an important technology for the development new functional molecules. Herein, a thioether‐mediated sulfenylation tryptophan (Trp)‐selective chemical under mild metal‐free reaction conditions involving weak acid/water solvent reported. An electrophilic species generated from 4‐fluorophenyl 3‐nitro‐2‐pyridinesulfenate, Npys‐OPh( p F), in presence thioether component, enables efficient Trp residue on various Trp‐containing biologically active linear cyclic peptides. In addition, this to late‐stage natural depsipeptide, daptomycin, expanded Trp‐sulfenylated derivatives, including fluorescent‐labeled are obtained. The results indicate that can be used robust Trp‐selective method wide range applications.

Язык: Английский