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).
Abstract: The present invention relates to a process for the preparation of a compound of formula (I) comprising the steps of a) reacting a compound of formula (II) with a silylating or an acylating agent to produce compound of formula (III), wherein P1 is a protecting group selected from R2—Si—R3R4 or R1CO—, 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) halogenation or sulfinylation of the compound of formula (III) to produce a compound of formula (IV); wherein X is halo, or —O—SO—R5, and R5 is a group selected from C6-10aryl or heteroaryl, each group being optionally substituted by one or more substituents independently selected from chloro or C1-4alkyl; c) dehalogenation or desulfinylation of t
Abstract: The present invention relates to a new use of tetrahydroxylated estrogens such as estetrol (1,3,5(10)-estratrien-3, 15?, 16?, 17?-tetrol), namely in a method of emergency contraception. The method of emergency contraception according to the invention comprises the oral administration of estetrol in a single dose within 120 hours of sexual intercourse.
Type:
Grant
Filed:
August 9, 2012
Date of Patent:
February 28, 2017
Assignee:
Estetra S.P.R.L.
Inventors:
Wout Wouters, Herman Jan Tijmen Coelingh Bennink, Ludivine Petit, Jean-Michel Foidart
Abstract: The present invention relates to a new use of tetrahydroxylated estrogens such as estetrol (1,3,5(10)-estratrien-3,15?,16?,17?-tetrol), namely in a method of emergency contraception. The method of emergency contraception according to the invention comprises the oral administration of estetrol in a single dose within 120 hours of sexual intercourse.
Type:
Application
Filed:
August 9, 2012
Publication date:
July 17, 2014
Applicant:
Estetra S.P.R.L.
Inventors:
Wout Wouters, Herman Jan Tijmen Coelingh Bennink, Ludivine Petit, Jean-Michel Foidart