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Radiosynthesis of 3 H‐ and 14 C‐labeled Veliparib
Author(s) -
Vaidyanathan Srirajan,
Reed Aimee,
Du Jia
Publication year - 2021
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3928
Subject(s) - veliparib , chemistry , radiosynthesis , adme , radiochemistry , cancer research , pharmacology , nuclear medicine , biochemistry , positron emission tomography , dna , medicine , polymerase , poly adp ribose polymerase , in vitro
Veliparib, a potent PARP inhibitor used against multiple cancerous cells such as metastatic melanoma, breast, non‐small cell lung cancer (NSCLC) and prostatic cancer, is required for absorption, distribution, metabolism and excretion (ADME) and environmental toxicology assessments studies. Tritium‐labeled Veliparib was prepared via the tritiodebromination using tritium gas (T 2 ) in two steps. [ 14 C]Veliparib was achieved through an asymmetric synthetic route in seven radioactive steps starting from [ 14 C] ( S )‐benzyl 2‐aminopropanoate.