Copper-Mediated Radiobromination of (Hetero)Aryl Boronic Pinacol Esters.
J Org Chem
; 88(4): 2089-2094, 2023 02 17.
Article
em En
| MEDLINE
| ID: mdl-36745853
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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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Cobre
/
Ésteres
Idioma:
En
Revista:
J Org Chem
Ano de publicação:
2023
Tipo de documento:
Article