3-¹⁸F-fluoropropane-1-thiol and ¹⁸F-PEG₄-1-thiol: Versatile prosthetic groups for radiolabeling maleimide functionalized peptides.

ABSTRACT: The efficient radiosynthesis of biomolecules utilizing minute quantities of maleimide substrate is important for availability of novel peptide molecular imaging agents. We evaluated both 3-¹⁸F-fluoropropane-1-thiol and 2-(2-(2-(2-¹⁸F-fluoroethoxy)ethoxy)ethoxy)ethane-1-thiol (¹⁸F-fluoro-PEG₄ thiol) as prosthetic groups for radiolabeling under physiological conditions. The precursor employed a benzoate for protection of the thiol and an arylsulfonate leaving group. The radiofluorination was fully automated on an Eckert & Ziegler synthesis system using standard Kryptofix₂₂₂/K₂CO₃ conditions. In order to minimize the amount of biological molecule required for subsequent conjugation, the intermediates, S-(3-¹⁸

SUBMITTER: Jacobson O 

PROVIDER: S-EPMC6983705 | biostudies-literature | 2019 Oct

REPOSITORIES: biostudies-literature