A fast, simple, and reproducible automated synthesis of [F-18]FPyKYNE-c(RGDyK) for alpha(v)beta(3) receptor positron emission tomography imaging

摘要

[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 >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.