15183-37-6Relevant articles and documents
Synthesis of 15α-hydroxyestrogen 15-N-acetylglucosaminides
Suzuki, Emako,Namba, Susumu,Kurihara, Hiroyuki,Goto, Junichi,Matsuki, Yasuhiko,Nambara, Toshio
, p. 277 - 284 (1995)
The synthesis of 15-N-acetylglucosaminides of 15α-hydroxyestrone, 15α-hydroxyestradiol, and 15α-hydroxyestriol (estetrol) is described.The latter two were prepared by condensation of 2-acetamido-1α-chloro-1,2-dideoxy-3,4,6-tri-O-acetyl-D-glucopyranose with appropriately protected 15α-hydroxyestrogens by the Koenigs-Knorr reaction employing cadmium carbonate as a catalyst.Subsequent removal of protecting groups with methanolic potassium hydroxide provided the desired conjugates. 15α-Hydroxyestrone 15-N-acetylglucosaminide was synthesized from the corresponding 15α-hydroxyestradiol derivative by Jones oxidation followed by brief alkaline hydrolysis.These conjugates underwent enzymatic hydrolysis with β-N-acetylglucosaminidase from Jack beans to produce 15α-hydroxyestrogens. - Keywords: 15α-hydroxyestrogen; N-acetylglucosaminide; Koenigs-Knorr reaction; 15-methoxyestrogen; β-N-acetylglucosaminidase
PROCESS FOR PREPARING (15ΑLPHA,16ΑLPHA,17ΒETA)-ESTRA-1,3,5(10)-TRIENE-3,15,16,17-TETROL (ESTETROL) AND INTERMEDIATES OF SAID PROCESS
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Page/Page column 14-15, (2021/04/02)
The present invention relates to a process for preparing (15α,16α,17β)-Estra-1,3,5(10)-triene-3,15,16,17-tetrol, also known as Estetrol, having the formula shown below: (I)
Process for the preparation of estetrol
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, (2011/11/12)
The present invention relates to a process for the preparation of estra-1,3,5(10)-trien-3,15α,16α,17β-tetraol (estetrol), 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, wherein A is a protecting group, via said silyl enol ether derivative.