(AZD9977), were prepared. Four stable isotope labeled versions of the compound were prepared for clinical bioanalysis and biological investigations. Three of these stable isotope labeled compounds were tritiated as well as the parent for biology applications and DMPK investigations. They were prepared using a standard iodination–tritiodehalogentation approach. Finally, AZD9977 was prepared in carbon-14 labeled
作为旨在发现用于治疗肾脏和心血管适应症的盐皮质激素受体调节剂的药物
化学计划的一部分,制备了先导化合物 balcinrenone (AZD9977) 的多种标记版本。制备了该化合物的四种稳定同位素标记形式用于临床
生物分析和
生物学研究。其中三种稳定同位素标记的化合物以及母体被氚化,用于
生物学应用和
DMPK 研究。它们是使用标准
碘化-三
硫代脱卤方法制备的。最后,AZD9977 被制备成碳 14 标记形式,用于临床前和临床应用。