Radiosynthesis of 3 H- and 14 C-labeled Veliparib

Abstract

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. [¹⁴ C]Veliparib was achieved through an asymmetric synthetic route in seven radioactive steps starting from [¹⁴ C] (S)-benzyl 2-aminopropanoate.

Keywords: C-14; Veliparib; absorption, distribution, metabolism and excretion (ADME); asymmetric synthesis; tritium.