Herstellung und Charakterisierung der Sulfamate von Estra-3,17xi-diolen. Schnelle Umsetzung von 16alpha-Fluorestradiol zum 16alpha-Fluorestradiol-3,17beta-disulfamat (Preparation and Characterization of the sulphamates of estra-3,17xi-diols. Rapid conversion of 16alpha-fluoroestradiol into 16alpha-fluoroestradiol-3,17beta-disulfamate)

Estradiols are able to form two monosulphamates and one disulphamate. In the present work all the sulphamates of 17alpha-estradiol, 17beta-estradiol and 16alpha-fluoroestradiol were synthesized and characterized. For characterization NMR spectroscopy was used first of all. Because of its high sulphatase inhibitory efficiency and 16alpha-fluoroestradiol-3,17beta-disulphamate found a special interest among the new sulphamates. Just the binding between sulphamate and sulphatase favoured 16alpha-[¹⁸F]fluorestradiol-3,17beta-disulphamate to a new radiopharmaceutical which should be appropriate to image the active sites of sulphatase by positron emission tomography. The preparation of 16alpha[¹⁸F]fluoroestradiol-3,17beta-disulphamate requires a simple and rapid procedure. The conditions for such a procedure were also elaborated using non-radioactive substances.