Synthesis of 18F-labelled cyclooxygenase-2 (COX-2) inhibitors via Stille reaction with 4-[18F]fluoroiodobenzene as radiotracers for positron emission tomography (PET).
The Stille reaction with 4-[(18)F]fluoroiodobenzene as a novel approach for the synthesis of radiotracers for monitoring COX-2 expression by means of PET has been developed. Optimized reaction conditions were elaborated by screening of various catalyst systems and solvents. By using optimized reaction conditions (18)F-labelled COX-2 inhibitors [(18)F]-5 and [(18)F]-13 could be obtained in radiochemical yields of up to 94% and 68%, respectively, based upon 4-[(18)F]fluoroiodobenzene.
Wüst
Frank R
FR
Institute of Bioinorganic and Radiopharmaceutical Chemistry, FZ-Rossendorf, PF 51 01 19, D-01314 Dresden, Germany. f.wuest@fz-rossendorf.de
Höhne
Aileen
A
Metz
Peter
P
D052246:Cyclooxygenase 2 Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D005462:Fluorine Radioisotopes / Q000737:chemistry*; D007462:Iodobenzenes / Q000737:chemistry*; D015394:Molecular Structure; D049268:Positron-Emission Tomography / Q000379:methods*; D011849:Radioactive Tracers
D052246:Cyclooxygenase 2 Inhibitors; D005462:Fluorine Radioisotopes; D007462:Iodobenzenes; D011849:Radioactive Tracers