213472-45-8Relevant academic research and scientific papers
Preparation and Characterization of the Sulphamates of Estra-3,17ξ-diols. Rapid Conversion of 16α-Fluoroestradiol into 16α-Fluoroestradiol-3,17β-disulphamate
Roemer,Steinbach,Kasch,Scheller
, p. 574 - 583 (2007/10/03)
Estradiols are able to form two monosulphamates and one disulphamate. In the present work all the sulphamates of 17α-estradiol, 17β-estradiol and 16α-fluoroestradiol were synthesized and characterized. For characterization NMR spectroscopy was used first of all. Because of its high sulphatase inhibitory efficiency 16α-fluoroestradiol-3,17-β-disulphamate found a special interest among the new sulphamates. Just the binding between sulphamate and sulphatase favoured 16α-[18F]fluorestradiol-3,17-β-disulphamate to a new radio-pharmaceutical which should be appropriate to image the active sites of sulphatase by positron emission tomography. The preparation of 16α-[18F]fluoroestradiol-3,17-β-disulphamate requires a simple and rapid procedure. The conditions for such a procedure were also elaborated using non-radioactive substances.
