Invention Grant
- Patent Title: Process for the production of estetrol intermediates
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Application No.: US14122872Application Date: 2012-06-01
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Publication No.: US11053274B2Publication Date: 2021-07-06
- Inventor: Jean-Claude Pascal
- Applicant: Jean-Claude Pascal
- Applicant Address: FR Nice
- Assignee: Jean-Claude Pascal
- Current Assignee: Jean-Claude Pascal
- Current Assignee Address: FR Nice
- Agency: Lathrop GPM LLP
- Agent James H. Velema, Esq.; Laura A. Labeots, Esq.
- Priority: EP11168561 20110601
- International Application: PCT/EP2012/060447 WO 20120601
- International Announcement: WO2012/164096 WO 20121206
- Main IPC: C07J1/00
- IPC: C07J1/00 ; C07J51/00 ; C07J13/00

Abstract:
The present invention relates to a process for the preparation of a compound of formula (I) said process comprising the steps of: a) reacting a compound of formula (II), with an acylating or a silylating agent to produce a compound of formula (III), wherein P1 and P2 are each independently a protecting group selected from R2—Si—R3R4, or R1CO—, wherein R1 is a group selected from C1-6alkyl or C3-6cycloalkyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; R2, R3 and R4 are each independently a group selected from C1-6alkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; b) reacting the compound of formula (III) in the presence of palladium acetate or a derivative thereof to produce compound of formula (IV); and c) reacting the compound of formula (IV) with a reducing agent to produce compound of formula (I).
Public/Granted literature
- US20140107358A1 PROCESS FOR THE PRODUCTION OF ESTETROL INTERMEDIATES Public/Granted day:2014-04-17
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