Direct 18F-Labeling of Biomolecules via Spontaneous Site-Specific Nucleophilic Substitution by F- on Phosphonate Prostheses.
Sign Up to like & getrecommendations! Published in 2021 at "Organic letters"
DOI: 10.1021/acs.orglett.1c01211
Abstract: We describe a high radiochemical yield late-stage direct 18F-labeling of bare biomolecules containing common active groups. Spontaneity and site-selectivity are attributed to the remarkably higher rates of nucleophilic substitution reactions on phosphonates than on other… read more here.
Keywords: nucleophilic substitution; 18f labeling; direct 18f; labeling biomolecules ... See more keywords
18F-Trifluoromethanesulfinate Enables Direct C–H 18F-Trifluoromethylation of Native Aromatic Residues in Peptides
Sign Up to like & getrecommendations! Published in 2020 at "Journal of the American Chemical Society"
DOI: 10.1021/jacs.9b11709
Abstract: 18F labeling strategies for unmodified peptides with [18F]fluoride require 18F-labeled prosthetics for bioconjugation more often with cysteine thiols or lysine amines. Here we explore selective radical chemistry to target aromatic residues applying C–H 18F-trifluoromethylation. We… read more here.
Keywords: aromatic residues; direct 18f; peptides 18f; 18f trifluoromethanesulfinate ... See more keywords