Synthesis of the taxane analogue PNU-105298 labelled with deuterium and with carbon-14

In this paper the preparations of the taxane analogue PNU-105298 (1), labelled with deuterium and with carbon-14 are described. A three-step sequence starting from the commercially available (tert-[H-2(9)]butyl)amine afforded the deuterium specifically labelled final compound [H-2(9)]PNU-105298 (1a). The preparation of the carbon-14 labelled final compound [C-14]PNU-105298 (1b) was carried out in a similar fashion yielding the radiochemically pure product with a specific activity of 2.15 GBq/mmol.