Synthesis of a 11C-labelled taxane derivative by (1- 11C)acetylation

摘要

The 11C-labelling of the taxane derivative BAY 59-8862 (1), a potent anticancer drug, was carried out as a module-assisted automated multi-step synthesis procedure. The radiotracer [11C]1 was synthesized by reacting [1-11C]acetyl chloride (6) with the lithium salt of the secondary hydroxy group of precursor 3 followed by deprotection. After HPLC purification of the final product [11C]1, its solid-phase extraction, formulation and sterile filtration, the decay-corrected radiochemical yield of [11C]1 was in the range between 12 and 23% (related to [11C]CO2; n = 10). The total synthesis time was about 54 min after EOB. The radiochemical purity of [11C]1 was greater than 96% and the chemical purity exceeded 80%. The specific radioactivity was 16.8 ± 4.7 GBq/μmol (n = 10) at EOS starting from 80 GBq of [11C]CO2. Copyright 2006 John Wiley & Sons, Ltd.