Department of Process Chemistry, Radiochemistry, AbbVie Inc, North Chicago, Illinois, USA.
J Labelled Comp Radiopharm. 2021 Jul;64(9):356-362. doi: 10.1002/jlcr.3928. Epub 2021 Jun 7.
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 ) in two steps. [ C]Veliparib was achieved through an asymmetric synthetic route in seven radioactive steps starting from [ C] (S)-benzyl 2-aminopropanoate.
用于吸收、分布、代谢和排泄 (ADME) 以及环境毒理学评估研究的 PARP 抑制剂维利帕尼(veliparib),对多种癌细胞如转移性黑色素瘤、乳腺癌、非小细胞肺癌(NSCLC)和前列腺癌具有治疗作用。通过使用氚气(T)进行两步氚代溴化反应制备氚标记维利帕尼。通过从[C](S)-苄基 2-氨基丙醇开始的七个放射性步骤的不对称合成路线,实现了[C]维利帕尼。