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Direct Fluorination Strategy for the Synthesis of Fluorine-18 Labeled Oligopeptide-[F-18]ApoPep-7

초록/요약 도움말

Knowing the extent to which apoptosis occurs will allow us to better understand physiological changes in cells. ApoPep-1, an oligopeptide with the structure of CQRPPR, is known to be a substance capable of measuring apoptosis well. A method for synthesizing ApoPep-1 derivative containing fluorine-18 was studied. The development of a method for labeling fluorine-18 fluorine on oligopeptide without denaturation of oligopeptide was applied to ApoPep-1. A derivative of ApoPep-1, a stable precursor 5 having trimethylammonium nicotinamide functional group was synthesized. The precursor 5 can be labeled at 40-60 degrees C without denaturing the oligopeptide to provide a new derivative, ApoPep-7 (1). Upon radiofluorination of the precursor 5 at 60 degrees C with large initial activity (11.2 GBq), [F-18]ApoPep-7 ([F-18]1) was obtained in a yield of 31% (nondecay corrected, isolated, total preparation time 65 min).

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