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Electrochemical platform improves alkyl bioisostere installation in drug development, suggesting new radiochemistry workflows.
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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Lin et al. (2025) studied this question.
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