Tritiation Of Azido-Labeled Diiodo Cabazitaxel (Jevtana) And Docetaxel (Taxotere) Derivatives To Generate H-3-Photoaffinity Probes
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS(2018)
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.
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关键词
azide reduction,cabazitaxel,docetaxel,I-D exchange,I-T exchange,photoaffinity probes,tritium-labeling
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