Mild Electrochemical Decarboxylative Giese Additions with Applications to <sup>18</sup> F‐Radiochemistry

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 18 F‐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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Publication Details

Journal
Advanced Synthesis & Catalysis
Published
2025-09-09
DOI
https://doi.org/10.1002/adsc.70113
Primary Topic
Synthesis and Biological Evaluation
Type
article
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article

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

Annie Ogasawara, G. K. Surya Prakash, Jeroen B. I. Sap, Jan Mařı́k et al.
Advanced Synthesis & Catalysis
Synthesis and Biological Evaluation
article

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

Annie Ogasawara, G. K. Surya Prakash, Jeroen B. I. Sap, Jan Mařı́k, Daniel Lin
article en

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 18 F‐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.

Advanced Synthesis & CatalysisVol. 367(21)
University of Southern California (US), Genesys (United States) (US)
Openalex Percentile: Top 81%
Synthesis and Biological Evaluation
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