Synthesis of 16alpha-[18F]fluorestradiol-3,17beta-disulphamate


Synthesis of 16alpha-[18F]fluorestradiol-3,17beta-disulphamate

Römer, J.; Füchtner, F.; Steinbach, J.

The synthesis of 16alpha-[18F]fluorestradiol-3,17beta-disulphamate ([18F]FESDS) is described. 16alpha-[18F]fluorestradiol ([18F]FES) is converted using excess sulphamoyl chloride in absolute acetonitrile in the presence of Kryptofix 2.2.2 and potassium carbonate using an automatically operating module. The required time for the synthesis related to end of bombardment is 3h, the maximum yield is 6%, and the maximum decay-corrected yield is 20%. The radiochemical purity of [18F]FESDS is > 99%. The specific radioactivity of [18F]FESDS is found to be between 150 and 200 GBq/µmol.

Keywords: 16alpha-[18F]fluorestradiol-3; 17beta-disulphamate; 18F-labelled tracer; positron emission tomography; sulphamoylation; HPLC purification

  • J. Labelled Cpd. Radiopharm. 43 (2000) 425-436

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