Rapid One-Step ¹⁸F‑Labeling of Peptides via Heteroaromatic Silicon-Fluoride Acceptors

A new class of organosilicon-based radiosynthons, heteroaromatic silicon-fluoride acceptors, namely, HetSiFAs, that readily undergo isotope exchange with dry [¹⁸F]­fluoride at room temperature in high radiochemical yield (up to 94%) with good molar activity is reported. Radiofluorination proceeds in a single step in 2 min without high-performance liquid chromatography purification to provide an operationally simple method for ¹⁸F-PET tracer production. This method was used to prepare an ¹⁸F-labeled commercial tetrapeptide, and positron emission tomography imaging confirmed in vivo stability.