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1. EP3240771 - PROCESS FOR THE PREPARATION OF OSPEMIFENE AND FISPEMIFENE

Office
European Patent Office
Application Number 15830869
Application Date 28.12.2015
Publication Number 3240771
Publication Date 08.11.2017
Publication Kind B1
IPC
C07C 43/23
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
43Ethers; Compounds having groups, groups or groups
02Ethers
20having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
23containing hydroxy or O-metal groups
C07C 41/16
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
41Preparation of ethers; Preparation of compounds having groups, groups or groups
01Preparation of ethers
16by reaction of esters of mineral or organic acids with hydroxy or O-metal groups
CPC
C07C 41/16
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
41Preparation of ethers; Preparation of compounds having groups, groups or groups
01Preparation of ethers
16by reaction of esters of mineral or organic acids with hydroxy or O-metal groups
C07C 43/23
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
43Ethers; Compounds having groups, groups or groups
02Ethers
20having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
23containing hydroxy or O-metal groups
Applicants OLON SPA
Inventors CRISTIANO TANIA
ALPEGIANI MARCO
Designated States
Priority Data MI20142267 29.12.2014 IT
Title
(DE) VERFAHREN ZUR HERSTELLUNG VON OSPEMIFEN UND FISPEMIFEN
(EN) PROCESS FOR THE PREPARATION OF OSPEMIFENE AND FISPEMIFENE
(FR) PROCÉDÉ DE PRÉPARATION D'OSPÉMIFÈNE ET DE FISPÉMIFÈNE
Abstract
(EN) Disclosed is a process for the synthesis of the active ingredients ospemifene and fispemifene which comprises reacting phenol 4 with an alkylating agent X- CH2CH2-Y of formula 7, wherein X is a leaving group and Y is the -(OCH2CH2)nOH group wherein n is zero or 1; or X and Y, taken together, represent an oxygen atom; to give ospemifene or fispemifene of formula 8.
(FR) L'invention concerne un procédé de synthèse des principes actifs que sont l'ospémifène et le fispémifène qui consiste à faire réagir le phénol (4) avec un agent alkylant X-CH2CH2-Y de formule (7), dans laquelle X représente un groupe partant et Y représente le groupe -(OCH2CH2)nOH dans lequel n représente zéro ou 1 ; ou X et Y représentent tous deux un atome d'oxygène ; afin d'obtenir l'ospémifène ou le fispémifène de formule 8.