Mild Electrochemical Decarboxylative Giese Additions with Applications to 18F‐Radiochemistry

IF 4 2区化学 Q2 CHEMISTRY, APPLIED

Advanced Synthesis & Catalysis Pub Date : 2025-09-09 DOI:10.1002/adsc.70113

Daniel Lin, Annie Ogasawara, Jan Marik, G. K. Surya Prakash, Jeroen Sap

引用次数: 0

Abstract

The incorporation of privileged saturated fragments into pharmaceutically relevant scaffolds has seen increased prevalence in drug discovery. Electrochemistry, a single‐electron enabling platform, has demonstrated remarkable synthetic potential, particularly in alkyl functionalizations. However, these two concepts have not yet been fully considered in 18F‐radiochemistry workflows. This work presents the development of a practical late‐stage electrochemical platform that utilizes mild conditions, low voltages, and applications toward the installation of rigid alkyl bioisosteres onto relevant drug scaffolds. The utility of this platform is further demonstrated in the electrochemical synthesis of a PARP1 radiotracer and its application in subsequent biodistribution studies.

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轻度电化学脱羧酶添加物及其在18F -放射化学中的应用

在药物发现中，将特权饱和片段纳入药学相关支架的现象越来越普遍。电化学，一个单电子使能平台，已经显示出显著的合成潜力，特别是在烷基功能化方面。然而，这两个概念尚未在18F‐放射化学工作流程中得到充分考虑。这项工作提出了一种实用的后期电化学平台的发展，该平台利用温和的条件，低电压，并应用于将刚性烷基生物异构体安装到相关药物支架上。该平台的实用性在PARP1放射性示踪剂的电化学合成及其在随后的生物分布研究中的应用中得到了进一步证明。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Advanced Synthesis & Catalysis 化学-应用化学

CiteScore

9.40

自引率

7.40%

发文量

447

审稿时长

1.8 months

期刊介绍： Advanced Synthesis & Catalysis (ASC) is the leading primary journal in organic, organometallic, and applied chemistry. The high impact of ASC can be attributed to the unique focus of the journal, which publishes exciting new results from academic and industrial labs on efficient, practical, and environmentally friendly organic synthesis. While homogeneous, heterogeneous, organic, and enzyme catalysis are key technologies to achieve green synthesis, significant contributions to the same goal by synthesis design, reaction techniques, flow chemistry, and continuous processing, multiphase catalysis, green solvents, catalyst immobilization, and recycling, separation science, and process development are also featured in ASC. The Aims and Scope can be found in the Notice to Authors or on the first page of the table of contents in every issue.