Invention Grant
- Patent Title: Process for the preparation of estetrol
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Application No.: US15022177Application Date: 2014-09-17
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Publication No.: US09988417B2Publication Date: 2018-06-05
- Inventor: Juan José Ferreiro Gil , Jesús Miguel Iglesias Retuerto , Francisco Javier Gallo Nieto
- Applicant: CRYSTAL PHARMA, S.A.U.
- Applicant Address: ES Boecillo-Valladolid
- Assignee: Crystal Pharma, S.A.U.
- Current Assignee: Crystal Pharma, S.A.U.
- Current Assignee Address: ES Boecillo-Valladolid
- Agency: Kramer Amado, P.C.
- Priority: EP13382360 20130918
- International Application: PCT/EP2014/069783 WO 20140917
- International Announcement: WO2015/040051 WO 20150326
- Main IPC: C07J1/00
- IPC: C07J1/00 ; C07J17/00

Abstract:
The invention relates to a process for obtaining Estetrol or a salt or solvate thereof, the process comprising: a) reacting a compound of formula (IV) or a salt or solvate thereof, wherein R1 is a hydroxyl protecting group selected from a silyl ether, an ether, an ester, a carbamate and a carbonate, and R2 is a hydroxyl protecting group selected from an ether, with an oxidizing agent selected from OsO4 or a source of osmium tetroxide to produce Estetrol or a compound of formula (II) or a salt or solvate thereof wherein R1 is as defined previously; and b) if a compound of formula (II) is obtained in step a), deprotecting said compound to produce Estetrol.
Public/Granted literature
- US20160229885A1 PROCESS FOR THE PREPARATION OF ESTETROL Public/Granted day:2016-08-11
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