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Direct Fluorination Strategy for the Synthesis of Fluorine‐18 Labeled Oligopeptide—[ 18 F ] ApoPep ‐7
Author(s) -
Oh Keumrok,
Chi Dae Yoon
Publication year - 2021
Publication title -
bulletin of the korean chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.237
H-Index - 59
ISSN - 1229-5949
DOI - 10.1002/bkcs.12350
Subject(s) - oligopeptide , chemistry , derivative (finance) , fluorine , stereochemistry , peptide , organic chemistry , biochemistry , financial economics , economics
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 °C without denaturing the oligopeptide to provide a new derivative, ApoPep‐7 ( 1 ). Upon radiofluorination of the precursor 5 at 60 °C with large initial activity (11.2 GBq), [ 18 F]ApoPep‐7 ([ 18 F] 1 ) was obtained in a yield of 31% (nondecay corrected, isolated, total preparation time 65 min).