Synthesis of 18F-labelled COX-2 inhibitors via Stille Reaction with 4-[18F]fluoro-iodobenzene.

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]- and [(18)F]- could be obtained in radiochemical yields of up to 94% and 68%, respectively, based upon 4-[(18)F]fluoroiodobenzene.