Clickable tryptophan modification for late-stage diversification of native peptides
Yisa Xiao,
Haiyan Zhou,
Pengfei Shi
et al.
Abstract:As the least abundant residue in proteins, tryptophan widely exists in peptide drugs and bioactive natural products and contributes to drug-target interactions in multiple ways. We report here a clickable tryptophan modification for late-stage diversification of native peptides, via catalyst-free
C
2-sulfenylation with 8-quinoline thiosulfonate reagents in trifluoroacetic acid (TFA). A wide range of groups including trifluoromethylthio (SCF
3
), difluoromethylthi… Show more
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