Automated synthesis of 16alpha-[18F]fluoroestradiol-3,17beta-disulphamate

Appl Radiat Isot. 2001 Nov;55(5):631-9. doi: 10.1016/s0969-8043(00)00339-0.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Arylsulfatases / antagonists & inhibitors
  • Enzyme Inhibitors / chemical synthesis
  • Estradiol / analogs & derivatives
  • Estradiol / chemical synthesis*
  • Fluorine Radioisotopes
  • Humans
  • Radiochemistry / instrumentation
  • Radiochemistry / methods
  • Radiopharmaceuticals / chemical synthesis*
  • Steryl-Sulfatase
  • Tomography, Emission-Computed

Substances

  • 16-fluoroestradiol-3,17-disulfamate
  • Enzyme Inhibitors
  • Fluorine Radioisotopes
  • Radiopharmaceuticals
  • Estradiol
  • Arylsulfatases
  • Steryl-Sulfatase