Radiosynthesis of 3H- and 14C-labeled Veliparib,Journal of Labelled Compounds and Radiopharmaceuticals

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Radiosynthesis of 3H- and 14C-labeled Veliparib
Journal of Labelled Compounds and Radiopharmaceuticals ( IF 0.9 ) Pub Date : 2021-05-29 , DOI: 10.1002/jlcr.3928
Srirajan Vaidyanathan ₁ , Aimee Reed ₁ , Jia Du ₁

Affiliation

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.

中文翻译：

3H 和 14C 标记的 Veliparib 的放射合成

Veliparib 是一种有效的 PARP 抑制剂，用于对抗多种癌细胞，如转移性黑色素瘤、乳腺癌、非小细胞肺癌 (NSCLC) 和前列腺癌，是吸收、分布、代谢和排泄 (ADME) 以及环境毒理学评估研究所必需的。氚标记的 Veliparib 通过使用氚气 (T ₂ ) 的氚脱溴作用分两步制备。 [ ¹⁴ C]Veliparib 是从[ ¹⁴ C] ( S )-2-氨基丙酸苄酯开始，通过不对称合成路线、七个放射性步骤获得的。

更新日期：2021-07-07

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