Last-step F-fluorination of supported 2-(aryl-di--butylsilyl)--methyl-imidazole conjugates for applications in positron emission tomography.

Aiming for potential applications in positron emission tomography, fully automated productions of F-labelled bioconjugates were achieved using heterogenous precursors obtained by anchoring imidazole-di--butyl-arylsilanes to a polystyrene resin. The reactions were performed using either "batch" or "flow" procedures, avoiding both the time-consuming azeotropic drying and HPLC purifications usually required.

Isotopic Radiolabeling of the Antiretroviral Drug [F]Dolutegravir for Pharmacokinetic PET Imaging.

Deciphering the drug/virus/host interactions at infected cell reservoirs is a key leading to HIV-1 remission for which positron emission tomography (PET) imaging using radiolabeled antiretroviral (ARV) drugs is a powerful asset. Dolutegravir (DTG) is one of the preferred therapeutic options to treat HIV and can be isotopically labeled with fluorine-18. [18F]DTG was synthesized via a three-step approach of radiofluorination/nitrile reduction/peptide coupling with optimization for each step.

Highly hindered 2-(aryl-di-tert-butylsilyl)-N-methyl-imidazoles: a new tool for the aqueous F- and F-fluorination of biomolecule-based structures.

A new class of silicon-based fluoride acceptors with a C-linked heterocycle as the leaving group was synthesized in one step from commercial chemicals, and linked to biomolecules. The resulting conjugates were efficiently 19F-fluorinated in aqueous mixtures, and switching to 18F-labelling provided nucleoside- and peptide-based bioconjugates with excellent molar activities suitable for biological applications.