Tritiation Of Azido-Labeled Diiodo Cabazitaxel (Jevtana) And Docetaxel (Taxotere) Derivatives To Generate H-3-Photoaffinity Probes

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS(2018)

引用 0|浏览4
暂无评分
摘要
Radiolabelled azidophenyl analogues can make powerful photoaffinity probes for the identification of molecular targets. We describe our efforts to prepare tritiated azidophenyl analogues of the taxols cabazitaxel and docetaxel. Late-stage tritiation by isotope exchange with diiodo precursors resulted in reduction of the azide moiety, which could only be overcome by addition of high excess of a sacrificial azide. Iodine-deuterium exchange experiments on a model system established that deiodination with concomitant azide reduction is a general problem when performing such isotope-exchange reactions on azide-containing aryl iodides.
更多
查看译文
关键词
azide reduction,cabazitaxel,docetaxel,I-D exchange,I-T exchange,photoaffinity probes,tritium-labeling
AI 理解论文
溯源树
样例
生成溯源树,研究论文发展脉络
Chat Paper
正在生成论文摘要