Rapid one-step 18F-radiolabeling of biomolecules in aqueous media by organophosphine fluoride acceptors

Huawei Hong, Lei Zhang, Fang Xie, Rongqiang Zhuang, Donglang Jiang, Huanhuan Liu, Jindian Li, Hongzhang Yang, Xianzhong Zhang, Liming Nie () and Zijing Li ()
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Huawei Hong: Xiamen University
Lei Zhang: Tianjin Chengjian University
Fang Xie: Fudan University
Rongqiang Zhuang: Xiamen University
Donglang Jiang: Fudan University
Huanhuan Liu: Xiamen University
Jindian Li: Xiamen University
Hongzhang Yang: Xiamen University
Xianzhong Zhang: Xiamen University
Liming Nie: Xiamen University
Zijing Li: Xiamen University

Nature Communications, 2019, vol. 10, issue 1, 1-7

Abstract: Abstract Currently, only a few 18F-radiolabeling methods were conducted in aqueous media, with non-macroelement fluoride acceptors and stringent conditions required. Herein, we describe a one-step non-solvent-biased, room-temperature-driven 18F-radiolabeling methodology based on organophosphine fluoride acceptors. The high water tolerance for this isotope-exchange-based 18F-labeling method is attributed to the kinetic and thermodynamic preference of F/F over the OH/F substitution based on computational calculations and experimental validation. Compact [18/19F]di-tert-butyl-organofluorophosphine and its derivatives used as 18F-labeling synthons exhibit excellent stability in vivo. The synthons are further conjugated to several biomolecular ligands such as c(RGDyk) and human serum albumin. The one-step labeled biomolecular tracers demonstrate intrinsic target imaging ability and negligible defluorination in vivo. The current method thus offers a facile and efficient 18F-radiolabeling pathway, enabling further widespread application of 18F.

Date: 2019
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DOI: 10.1038/s41467-019-08953-0

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