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Published on: November 30, 2022
Copper-Mediated Radiobromination of (Hetero)Aryl Boronic Pinacol Esters
Jason C Mixdorf1, Sabrina L V Hoffman1, Eduardo Aluicio-Sarduy1
1Department of Medical Physics, University of Wisconsin School of Medicine and Public Health, 1111 Highland Avenue, Madison, Wisconsin 53705, United States.
Abstract:
A copper-mediated radiobromination of (hetero)aryl boronic pinacol esters is described. Cyclotron-produced [76/77Br]bromide was isolated using an anion exchange cartridge, wherein the pre-equilibration and elution solutions played a critical role in downstream deboro-bromination. The bromination tolerates a broad range of functional groups, labeling molecules with ranging electronic and steric effects. Bologically active radiopharmaceuticals were synthesized, including two radiobrominated inhibitors of poly ADP ribose polymerase, a clinically relevant chemotherapeutic target for ovarian, breast, and prostate cancers.
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