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The first application of sulfo-click chemistry with 18F-labeled thio acids is described. The simple one-pot/three-component reaction proceeded rapidly within 30 min using mild reaction conditions to give various 18F-labeled small molecule N-acylsulfonamides in radiochemical conversions of 38–99%, and radiolabeled peptides in 20–25% isolated and decay-corrected radiochemical yields. [ABSTRACT FROM AUTHOR]

The study describes the Sonogashira cross-coupling reaction with 4-[18F]fluoroiodobenzene ([18F]FIB) as novel and efficient method for rapid labelling of peptides with the short-lived positron emitter fluorine-18. [ABSTRACT FROM AUTHOR]

The ketone bodies d-beta-hydroxybutyric acid and acetoacetic acid represent the principal oxidative energy sources of most tissues when dietary glucose is scarce. An 18 F-labeled ketone body could be a useful tool for studying ketone body metabolism using positron emission tomography (PET). Here, we report the first radiofluorinated ketone body derivative (3 S )-4-[ 18 F]fluoro-3-hydroxybutyric acid ([ 18 F]FBHB) as well as its enantiomer and l-beta-hydroxybutyric acid derivative, (3 R )-4-[ 18 F]fluoro-3-hydroxybutyric acid (( R )-[ 18 F]F3HB). PET imaging in mice showed biodistribution profiles of the radiotracers that were consistent with the biodistribution of the respective endogenous compounds. Moreover, both enantiomers visualized breast cancer xenografts in vivo . Fasting over 24 h showed significantly enhanced brain and heart uptake of [ 18 F]FBHB and tumor uptake of ( R )-[ 18 F]F3HB. Disorders exhibiting altered energy substrate utilization, such as Alzheimer's disease, epilepsy, diabetes, and cancer may be of interest for PET imaging studies using [ 18 F]FBHB., (This journal is © The Royal Society of Chemistry 2020.)

The first application of sulfo-click chemistry with 18F-labeled thio acids is described. The simple one-pot/three-component reaction proceeded rapidly within 30 min using mild reaction conditions to give various 18F-labeled small molecule N-acylsulfonamides in radiochemical conversions of 38-99%, and radiolabeled peptides in 20-25% isolated and decay-corrected radiochemical yields.

The study describes the Sonogashira cross-coupling reaction with 4-[(18)F]fluoroiodobenzene ([(18)F]FIB) as novel and efficient method for rapid labelling of peptides with the short-lived positron emitter fluorine-18.