Direct Fluorination Strategy for the Synthesis of Fluorine-18 Labeled Oligopeptide—[18F]ApoPep-7,Bulletin of the Korean Chemical Society

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Direct Fluorination Strategy for the Synthesis of Fluorine-18 Labeled Oligopeptide—[18F]ApoPep-7
Bulletin of the Korean Chemical Society ( IF 2.3 ) Pub Date : 2021-07-06 , DOI: 10.1002/bkcs.12350
Keumrok Oh ₁ , Dae Yoon Chi ₁

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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), [¹⁸F]ApoPep-7 ([¹⁸F]1) was obtained in a yield of 31% (nondecay corrected, isolated, total preparation time 65 min).

中文翻译：

用于合成氟 18 标记寡肽的直接氟化策略 - [18F]ApoPep-7

了解细胞凋亡发生的程度将使我们能够更好地了解细胞的生理变化。ApoPep-1是一种具有CQRPPR结构的寡肽，已知是一种能够很好地测量细胞凋亡的物质。研究了一种合成含氟18的ApoPep-1衍生物的方法。在不使寡肽变性的情况下在寡肽上标记氟-18 氟的方法的开发应用于 ApoPep-1。合成了 ApoPep-1 的衍生物，一种具有三甲基烟酰胺官能团的稳定前体5。前体5可以在 40–60 °C 下标记，而不会使寡肽变性以提供新的衍生物 ApoPep-7 ( 1 )。前体5 的放射性氟化后在 60 °C 下以大的初始活性 (11.2 GBq)，以 31% 的产率获得[ ¹⁸ F]ApoPep-7 ([ ¹⁸ F] 1 )（未衰减校正，分离，总制备时间 65 分钟）。

更新日期：2021-08-19

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