18 F-Fluorination of a supported 2-(aryl-di-tert-butylsilyl)-N-methyl-imidazole for indirect 18 F-labeling of a VH H single-variable domain.

Anchoring an imidazole-di-tert-butyl-arylsilane possessing an azido group to a polystyrene resin provided a heterogeneous precursor that was radiolabeled easily using aqueous [18 F]fluoride. After optimizing the conditions (i.e., using DMSO as solvent and heating at 160°C for 15 min), the desired [18 F]fluorosilane was obtained in 24% radiochemical yield (RCY) and 78% radiochemical purity (RCP) using solid-phase extraction as sole purification. Then, this compound was conjugated by strain-promoted alkyne-azide cycloaddition to a model single-variable domain possessing a cyclooctyne tag, yielding to the desired 18 F-labeled bioconjugate in 2% RCY and >95% RCP after purification by a size exclusion chromatography.

Last-step 18F-fluorination of supported 2-(aryl-di-tert-butylsilyl)-N-methyl-imidazole conjugates for applications in positron emission tomography.

Aiming for potential applications in positron emission tomography, fully automated productions of 18F-labelled bioconjugates were achieved using heterogenous precursors obtained by anchoring imidazole-di-tert-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.