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对于的化学选择性F标记而使用的脱氧化

Riya Halder^1,2, Gaoyuan Ma^3,4, Jens Rickmeier¹

¹Department of Organic Synthesis, Max-Planck-Institut für Kohlenforschung, Mülheim an der Ruhr, Germany.

Nature protocols

|October 18, 2023

概括

开发新的-18标记的PET成像剂是具有挑战性的. 本研究介绍了两种新的放射性氧化化方法来合成18F-烯化物,使得对正电子发射断层扫描 (PET) 研究的有效标记成为可能.

科学领域:

放射化学放射化学是指辐射化学.
药用化学医学化学
生物结合的生物结合

背景情况:

形成碳-18F键是开发新型正子发射断层扫描 (PET) 追踪器的关键瓶.
目前用于18F标签的核芳香替代方法仅限于缺乏电子的,并且与许多功能群不兼容,特别是在敏感的基质中.
基于的PET成像探头是非常理想的,但由于18F结合的挑战,很难合成.

研究的目的:

开发新的,广泛适用的放射性氧化化方法来合成18F-烯化物.
为 PET 成像实现高密度功能化的高效和化学选择性标记.
提供与现有放射合成设备兼容的自动化和实用的放射标记程序.

主要方法:

两种相辅相成的放射性氧化化方法被开发用于实验室稳定的.
方法1:合成一个18F-synthon和随后的绑定到Arg-Gly-Asp-Cys.
方法2:固相合成,采用改性氨酸,然后通过以18F为媒介的鲁脱氧化和脱保护.

主要成果:

这两种方法都能快速获得富含电子和缺乏电子的18F-烯化物.
方法1在10.5小时 (189分钟放射合成) 中实现了Arg-Gly-Asp-Cys的标记.
方法2在7天内 (116分钟放射合成) 产生了标记的,并显示出高化学选择性和自动化兼容性.

结论:

开发的放射性氧化化策略显著扩大了复杂分子18F标签的实用性.
这些方法促进了基于的PET探针的合成,使得体内成像研究成为可能.
这些程序的自动化支持PET标记器开发的尽可能低的合理可实现 (ALARA) 原则.

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