Automated synthesis of 16alpha-[18F]fluoroestradiol-3,17beta-disulphamate.
After 16alpha-[15F]fluoroestradiol ([18F]FES) has been successfully prepared in an automated module, the synthesis of 16alpha-[18F]fluoroestradiol-3,17beta-disulphamate ([18F]FESDS) is described as a module-assisted one-pot procedure which can provide 10GBq [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 [15F]FESDS is thought to be a new PET tracer to image sites of high sulphatase activity.
Römer
J
J
Forschungszentrum Rossendorf e.V., Institut für Bioanorganische und Radiopharmazeutische Chemie, Dresden, Germany. j.roemerj@fz-rossendorf.de
Füchtner
F
F
Steinbach
J
J
Kasch
H
H
D001192:Arylsulfatases / Q000037:antagonists & inhibitors; D004791:Enzyme Inhibitors / Q000138:chemical synthesis; D004958:Estradiol / Q000031:analogs & derivatives / Q000138:chemical synthesis*; D005462:Fluorine Radioisotopes; D006801:Humans; D011854:Radiochemistry / Q000295:instrumentation / Q000379:methods; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D043266:Steryl-Sulfatase; D014055:Tomography, Emission-Computed
C441859:16-fluoroestradiol-3,17-disulfamate; D004791:Enzyme Inhibitors; D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; D004958:Estradiol; D001192:Arylsulfatases; D043266:Steryl-Sulfatase