Abstract
AbstractThis work describes the synthesis and 18F‐labeling of an amino acid based prosthetic group that is able to participate in copper(I)‐catalyzed cycloadditions. The prosthetic group can be used for 18F labeling of biomolecules under mild conditions. The synthesis started with L‐serine methyl ester, which was derivatized by introducing an alkyne moiety and a leaving group for 18F labeling. Subsequently, 18F labeling as well as deprotection conditions were screened, which resulted in an overall radiochemical yield (RCY) of around 28 %. Furthermore, the 18F‐labeled prosthetic group was treated with an azido cyclic Arg‐Gly‐Asp (cRGD) peptide as a model system in very high RCY of 98 %.
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