SYNTHESIS OF A ~(11)C-LABELLED TAXANE DERIVATIVE BY [l-~(11)C]ACETYLATION

摘要

Taxanes are an important class of antitumor agents. These compounds bind to the microtubuli and inhibit their depolymerization into tubulin. Subsequently, the mitosis is disrupted and the cells are not able to divide into daughter cells.1 Investigations with positron emission tomography (PET) are an important tool to determine the in vivo distribution and the pharmacoki-netics of such drugs when they are labelled with positron-emitting radio-nuclides. An example for such a labelling is the synthesis of [~(11)C]paclitaxel by reacting [carbonyl-~(11)C]benzoyl chloride with the corresponding primary amine precursor. Paclitaxel (Taxol) is an effective anticancer drug against solid tumors.