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, 17ß-tetraol (estetrol), via a silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-l,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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Hauptverfasser: COELINGH BENNINK, HERMAN JAN TIJMEN, VAN VLIET, MICHIEL CHRISTIAN ALEXANDER, PLATTEEUW, JOHANNES JAN, DAMEN, FRANCISCUS WILHELMUS PETRUS
Format: Patent
Sprache:eng ; fre
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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, 17ß-tetraol (estetrol), via a silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-l,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, wherein A is a protecting group, via said silyl enol ether derivative.