Automated synthesis of 16α-[18F]fluoroestradiol-3,17β-disulphamate

After 16α-[18F]fluoroestradiol ([18F]FES) has been successfully prepared in an automated module, the synthesis of 16α-[18F]fluoroestradiol-3,17β-disulphamate ([18F]FESDS) is described as a module-assisted one-pot procedure which can provide 10 GBq [18F]FESDS with a radiochemical purity better than 99%. The procedure is reliable and reproducible and requires a time of about 90 min. Because of its high sulphatase-inhibitory effect [18F]FESDS is thought to be a new PET tracer to image sites of high sulphatase activity.