Radiosynthesis of 3H‐ and 14C‐labeled Veliparib

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‐l...

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Bibliographic Details
Published in:Journal of labelled compounds & radiopharmaceuticals 2021-07, Vol.64 (9), p.356-362
Main Authors: Vaidyanathan, Srirajan, Reed, Aimee, Du, Jia
Format: Article
Language:English
Subjects:
absorption, distribution, metabolism and excretion (ADME)
asymmetric synthesis
Breast
C‐14
Melanoma
Metastases
Non-small cell lung carcinoma
Poly(ADP-ribose) polymerase
Small cell lung carcinoma
Toxicology
Tritium
Veliparib
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Summary: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 (T2) in two steps. [14C]Veliparib was achieved through an asymmetric synthetic route in seven radioactive steps starting from [14C] (S)‐benzyl 2‐aminopropanoate. 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 ADME and environmental toxicology assessments studies. Tritium‐labeled Veliparib was prepared via the tritiodebromination using tritium gas (T2) in two steps. [14C]Veliparib was achieved through an asymmetric synthetic route in seven radioactive steps starting from [14C] (S)‐benzyl 2‐aminopropanoate.
ISSN:0362-4803
1099-1344
DOI:10.1002/jlcr.3928