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

Maruthi Kumar NarayanamAnton A ToutovJennifer M Murphy
Published in: Organic letters (2020)
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.
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