氧化银介导的烷基双聚18f -二氟烷基基序的放射化学合成

IF 5 1区化学 Q1 CHEMISTRY, ORGANIC

Organic Letters Pub Date : 2025-02-06 DOI:10.1021/acs.orglett.5c00187

Pawan Mishra, Jasmine Hind, Ian A. Fallis, Matthew Tredwell

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引用次数: 0

摘要

18F放射性示踪剂用于医学诊断和药物开发的正电子发射断层成像。目前合成18f -多氟官能团的方法在底物范围上受到限制，并且产生低摩尔活性（Am）的放射性示踪剂。我们揭示了通过Ag2O介导的[18F]氟取代双溴氟烷基亲核试剂来合成一系列18F-二氟烷基。这种转换对支持（预）临床成像的效用通过转换到自动合成器来证明。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Radiochemical Synthesis of Alkyl Geminal 18F-Difluoroalkyl Motifs Mediated by Silver(I) Oxide

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Radiochemical Synthesis of Alkyl Geminal 18F-Difluoroalkyl Motifs Mediated by Silver(I) Oxide

¹⁸F radiotracers are used in positron emission tomography imaging for medical diagnosis and drug development. Current methods to synthesize ¹⁸F-polyfluorinated functional groups are limited in substrate scope and result in radiotracers with low molar activities (A_m). We disclose the synthesis of a range of ¹⁸F-difluoroalkyl groups by nucleophilic substitution of geminal bromofluoroalkyl electrophiles with [¹⁸F]fluoride mediated by Ag₂O. The utility of this transformation to support (pre)clinical imaging is demonstrated by translation to an automated synthesizer.

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来源期刊

Organic Letters 化学-有机化学

CiteScore

9.30

自引率

11.50%

发文量

1607

审稿时长

1.5 months

期刊介绍： Organic Letters invites original reports of fundamental research in all branches of the theory and practice of organic, physical organic, organometallic,medicinal, and bioorganic chemistry. Organic Letters provides rapid disclosure of the key elements of significant studies that are of interest to a large portion of the organic community. In selecting manuscripts for publication, the Editors place emphasis on the originality, quality and wide interest of the work. Authors should provide enough background information to place the new disclosure in context and to justify the rapid publication format. Back-to-back Letters will be considered. Full details should be reserved for an Article, which should appear in due course.