Process for the preparation of estetrol

The present invention relates to a process for the preparation of estra-1,3,5(10)-trien-3, 15a, 16a, 17β-tetraol (estetr-01), via a silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10), 16-tetraene, wherein A is a protecting group and B is -Si(R2)3. The invention further relates to a process...

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Bibliographische Detailangaben
Hauptverfasser: Van Vliet, Michiel Christian Alexander, Platteeuw, Johannes Jan, Coelingh Bennink, Herman Jan Tijmen, Damen, Franciscus Wilhelmus Petrus
Format: Patent
Sprache:eng
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Zusammenfassung:The present invention relates to a process for the preparation of estra-1,3,5(10)-trien-3, 15a, 16a, 17β-tetraol (estetr-01), via a silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10), 16-tetraene, wherein A is a protecting group and B is -Si(R2)3. The invention further relates to a process for the synthesis of 3-A-oxy-estra-1,3,5(10), 15-tetraen-17-one, in which A is a protecting group, via silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10),16-tetraene, and B is -Si(R2)3.