Sultones for Radiofluorination and Bioconjugation: Fluorine-18 Labeling of Native Proteins and Glycoproteins [PDF]
Aliphatic nucleophilic substitution of a sulfonate ester group (such as triflate, mesylate, tosylate, or nosylate) represents a prominent reaction in fluorine-18 chemistry, as illustrated by the radiosynthesis of [18F]FDG (fluorodeoxyglucose) routinely ...
Anne-Elodie Lafargue +4 more
doaj +4 more sources
Generic semi-automated radiofluorination strategy for single domain antibodies: [18F]FB-labelled single domain antibodies for PET imaging of fibroblast activation protein-α or folate receptor-α overexpression in cancer [PDF]
Background Radiofluorination of single domain antibodies (sdAbs) via N-succinimidyl-4-[18F]fluorobenzoate ([18F]SFB) has shown to be a promising strategy in the development of sdAb-based PET tracers. While automation of the prosthetic group (PG) [18F]SFB
Herlinde Dierick +11 more
doaj +5 more sources
Bifunctional Hexadentate Pyclen-Based Chelating Agent for Mild Radiofluorination in Aqueous Solution at Room Temperature with a Ga-18F Ternary Complex. [PDF]
Positron Emission Tomography (PET) is used in oncology for tumor diagnosis, commonly relying on fluorine‐18 (18F) emission detection. The conventional method of 18F incorporation on to probes by covalent bonding is harsh for sensitive biomolecules, which
Dioury F +10 more
europepmc +5 more sources
Lewis Acid-Facilitated Radiofluorination of MN3PU: A LRRK2 Radiotracer [PDF]
Background: Temperature-sensitive radiopharmaceutical precursors require lower reaction temperatures (
Noeen Malik +3 more
doaj +4 more sources
The hydrogenation side-reaction in copper-mediated radiofluorination [PDF]
Background Copper-mediated radiofluorination (CMRF) is a breakthrough in 18F-radiochemistry, enabling 18F incorporation into molecules even at electron-rich aromatic positions. In recent years, several improved protocols have been reported to advance the
Sarandeep Kaur +5 more
doaj +3 more sources
A simplified, robust protocol for [18F]fluoride elution under mild conditions to enhance late-stage aromatic radiofluorinations [PDF]
Direct radiofluorination of base-sensitive PET precursors is challenging due to the harsh reaction conditions of traditional fluorine-18 radiochemistry. In particular, the presence of inorganic bases with a relatively high conjugate pK a (e.g. K2CO3) and
Stefan Milton +4 more
doaj +4 more sources
Manufacturing 6-[<sup>18</sup>F]Fluoro-<i>L</i>-DOPA via Flow Chemistry-Enhanced Photoredox Radiofluorination. [PDF]
In this study, we introduce a practical methodology for the synthesis of PET probes by seamlessly combining flow chemistry with photoredox radiofluorination.
Wu X +6 more
europepmc +4 more sources
Automated radiofluorination of HER2 single domain antibody: the road towards the clinical translation of [18F]FB-HER2 sdAb [PDF]
Background With the next generation of Human Epidermal Growth Factor Receptor 2 (HER2) -targeting therapies, such as antibody–drug conjugates, showing benefit in “HER2 low” and even “HER2 ultralow” patients, the need for novel methods to quantify HER2 ...
Herlinde Dierick +6 more
doaj +3 more sources
Arene radiofluorination enabled by photoredox-mediated halide interconversion [PDF]
Abstract Positron emission tomography (PET) is a powerful imaging technology that could visualize and measure metabolic processes in vivo and/or obtain unique information about drug candidates at early stages. Identification of new and improved molecular probes plays a critical role in PET, but its progress is limited in many situations due to ...
Wei Chen +8 more
openalex +4 more sources
Strained Ammonium Precursors for Radiofluorinations
AbstractThe increasing application of positron emission tomography (PET) in nuclear medicine has stimulated the extensive development of a multitude of novel and versatile techniques to introduce fluorine‐18, especially for the radiolabelling of biologically or pharmacologically active molecules.
Falco Reissig, Constantin Mamat
openalex +5 more sources

