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.

译文

目前,在非大分子氟化物受体和严格的条件下,在水性介质中仅进行了几种18f放射性标记方法。在这里,我们描述了一种基于有机膦氟化物受体的一步非溶剂偏置,室温驱动的18f放射性标记方法。基于计算计算和实验验证,这种基于同位素交换的18f标记方法的高耐水性归因于F/F相对于OH/F取代的动力学和热力学偏好。紧凑型 [18/19F] 二叔丁基-有机氟膦及其用作18f-标记合成子的衍生物在体内表现出优异的稳定性。该合成子进一步与几个生物分子配体如c(RGDyk) 和人血清白蛋白偶联。一步标记的生物分子示踪剂展示了内在的靶成像能力和可忽略的体内脱氟。因此,当前的方法提供了一种简便有效的18f放射性标记途径,使18F进一步广泛应用。

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