Improved and semi-automated GMP-compliant radiosynthesis of [11C]docetaxel

[11C]Docetaxel (Taxotere®) has been synthesized via an improved synthesis route, which involves a more efficient intermediate removal of the excess 1,2,2,2-tetrachloroethyl chloroformate. Furthermore, the purification and formulation into a human applicable solution of [11C]docetaxel was developed. 1,2,2,2-Tetrachloroethyl chloroformate is used for the synthesis of the intermediate [11C]tert-butyl-1,2,2,2-tetrachloroethyl carbonate that in the final reaction step reacts with the precursor, the primary amine of docetaxel, yielding [11C]docetaxel. The purified and isolated product was obtained in 10±2% overall decay-corrected radiochemical yield. The total synthesis time was 67 min and the specific activity was 9–17 GBq/μmol (N=7).