A fast, simple, and reproducible automated synthesis of [¹⁸F]FPyKYNE‐c(RGDyK) for <i>α</i>_v<i>β</i>₃ receptor positron emission tomography imaging

Abstract

[ 18 F]FPyKYNE‐c(RGDyK) was successfully synthesized by the Cu(I) catalyzed Huisgen 1,3‐dipolar cycloaddition of alkynes to azides using [ 18 F]FPyKYNE as a prosthetic group in an overall radiochemical yield of 12%–18% (decay‐corrected) and &gt;99.5% chemical and radiochemical purities in 125 min including quality control. This simple, fully automated two‐step, two‐reactor approach consists of a quick and convenient purification of the prosthetic group using silica gel cartridges and its subsequent use for the labeling of the azido‐c(RGDyK) peptide via click chemistry.