Journal
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
Volume 55, Issue 2, Pages 57-60Publisher
WILEY-BLACKWELL
DOI: 10.1002/jlcr.1948
Keywords
av ss 3 integrin receptors; 18F-labeling; [18F]-FPyKYNE; c(iRGDyK); PET
Funding
- Heart and Stroke Foundation of Ontario (HSFO GIA) [PGR6242]
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[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.
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