Versatile Pyridinium Trifluoroborate Platform for Facile Preparation of 18F-Labeled PET Tracers in Water

IF 11.1 1区化学 Q1 CHEMISTRY, MULTIDISCIPLINARY

ACS Central Science Pub Date : 2026-06-24 Epub Date: 2026-05-06 DOI:10.1021/acscentsci.6c00164

Wei Li, Yi Li, Tiyi Lyu, Yu Chen, Jingjing Ma*, Yi Fang* and Li Zhang*,

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引用次数: 0

Abstract

[¹⁸F]-Organotrifluoroborate salts are important radioprosthetic groups for positron emission tomography (PET) imaging. However, their application is hindered by hydrolytic instability in vivo. Several water-tolerant trifluoroborate scaffolds have been developed, but their multistep syntheses restrict structural diversity. Consequently, access to water-stable organotrifluoroborates with broad structural and physicochemical variation remains a challenge. Herein, a library of water-stable trifluoroborate reagents for PET tracer preparation has been developed. The reagents feature one-step synthesis, structural diversity, and high stability under aqueous conditions. The hydrolysis-resistant feature of the reagents enables the preparation of PET tracer precursors in water. Facile ¹⁸F–¹⁹F isotope exchange reactions facilitate the preparation of diverse PET tracers with pyridinium [¹⁸F]BF₃ prosthetic groups.

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多功能三氟硼酸吡啶平台，用于在水中快速制备18f标记的PET示踪剂

[18F]-有机三氟硼酸盐是正电子发射断层扫描（PET）成像中重要的放射性修复基团。然而，它们的应用受到体内水解不稳定性的阻碍。几种耐水三氟硼酸酯支架已经开发出来，但它们的多步骤合成限制了结构的多样性。因此，获得具有广泛结构和物理化学变化的水稳定型有机三氟硼酸盐仍然是一项挑战。在此，开发了用于制备PET示踪剂的水稳定三氟硼酸试剂库。该试剂具有一步合成、结构多样、在水环境下稳定性高的特点。试剂的抗水解特性使在水中制备PET示踪前体成为可能。简单的18F - 19f同位素交换反应有助于用吡啶[18F]BF3假基制备各种PET示踪剂。

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来源期刊

ACS Central Science Chemical Engineering-General Chemical Engineering

CiteScore

25.50

自引率

0.50%

发文量

194

审稿时长

10 weeks

期刊介绍： ACS Central Science publishes significant primary reports on research in chemistry and allied fields where chemical approaches are pivotal. As the first fully open-access journal by the American Chemical Society, it covers compelling and important contributions to the broad chemistry and scientific community. "Central science," a term popularized nearly 40 years ago, emphasizes chemistry's central role in connecting physical and life sciences, and fundamental sciences with applied disciplines like medicine and engineering. The journal focuses on exceptional quality articles, addressing advances in fundamental chemistry and interdisciplinary research.