Microfluidic reactions using [~(11)C]lcarbon monoxide solutions for the synthesis of a positron emission tomography radiotracer

摘要

Microfluidic technology has been used to perform [~(11)C]carbonylation reactions using solutions containing [~(11)C]CO in the form of the complex, copper(I)tris(3,5-dimethylpyrazolyl)borate-[~(11)C]carbonyl (Cu(Tp*)[~(11)C]CO). The synthesis of the model compound [~(11)C]V-benzylbenzamide and the known tracer molecule [~(11)C]trans-N-[5-(2-flurophenyl)-2-pyrimidinyl]-3-oxospiro[5-azaisobenzofurane-l(3H),l'-cyclohexane]-4'-carboxamide ([~(11)C]MK-0233), a ligand for the neuropeptide Y Y5 receptor, have been performed using this technique. Following semi-preparative HPLC purification and reformulation, 1262 + 113 MBq of [~(11)CJMK-0233 was produced at the end of the synthesis with a specific activity of 100 ± 30 GBq μmol~(-1) and a >99% radiochemical purity. This corresponds to a decay corrected radiochemical yield of 7.2 ± 0.7%. Using a 3 mL vial as the reaction vessel, and following semi-preparative HPLC purification and reformulation, 1255 + 392 MBq of [~(11)C]MK-0233 was produced at the end of the synthesis with a specific activity of 100+15 GBq μmol~(-1) and a >99% radiochemical purity. This corresponds to a decay corrected radiochemical yield of 7.1 ± 2.2%.