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Proxy-Pet Building Blocks As A Design Element For Library Synthesis, Lainey Jo Mallin
Proxy-Pet Building Blocks As A Design Element For Library Synthesis, Lainey Jo Mallin
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In exploring radioligands for positron emission tomography (PET) imaging, it is not unusual to synthesize a library of compounds around some targeting scaffold, screen for optimal binding to a relevant diagnostic cellular target, remove some portion of optimized molecule so as to append the requisite reporter group, and then re-evaluate. To this end, the use of "click labeling" in radiochemistry is proving an increasingly attractive means of conjugating a 18F-reporter group, wherein the targeting scaffold bearing a terminal alkyne is allowed to react with a 2-[18F]-fluoroethylazide to forge a linkage as a 1,2,3-triazole substituent. Since the triazole linked prosthetic group …