title: Microfluidic reactions using [11C]carbon monoxide solutions for the synthesis of a positron emission tomography radiotracer.
abstract: 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]N-benzylbenzamide and the known tracer molecule [(11)C]trans-N-[5-(2-flurophenyl)-2-pyrimidinyl]-3-oxospiro[5-azaisobenzofurane-1(3H),1'-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)C]MK-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%.
authors: GlaxoSmithKline Clinical Imaging Centre, Hammersmith Hospital, London, W12 0NN, UK.
authors: Steven
authors: S
authors: Kealey
authors: Christophe
authors: C
authors: Plisson
authors: T Lee
authors: TL
authors: Collier
authors: Nicholas J
authors: NJ
authors: Long
authors: Stephen M
authors: SM
authors: Husbands
authors: Laurent
authors: L
authors: Martarello
authors: Antony D
authors: AD
authors: Gee
mesh_terms: D002248:Carbon Monoxide / Q000138:chemical synthesis*; D002250:Carbon Radioisotopes / Q000737:chemistry; D046210:Microfluidic Analytical Techniques; D044085:Microfluidics; D015394:Molecular Structure; D049268:Positron-Emission Tomography; D011849:Radioactive Tracers; D012996:Solutions / Q000737:chemistry
chemical_list: D002250:Carbon Radioisotopes; D011849:Radioactive Tracers; D012996:Solutions; D002248:Carbon Monoxide