WO2016108172 PROCESS FOR THE PREPARATION OF OSPEMIFENE AND FISPEMIFENE

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Publication Number WO/2016/108172

Publication Date 07.07.2016

International Application No. PCT/IB2015/060007

International Filing Date 28.12.2015

IPC

CPC

Applicants

OLON S.P.A. [IT]/[IT]

Inventors

CRISTIANO, Tania
ALPEGIANI, Marco

Agents

MINOJA, Fabrizio

Priority Data

MI2014A002267

29.12.2014

Publication Language English (en)

Filing Language Italian (IT)

Designated States

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Title

(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.

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
C	ACYCLIC OR CARBOCYCLIC COMPOUNDS
41	Preparation of ethers; Preparation of compounds having groups, groups or groups
01	Preparation of ethers
16	by reaction of esters of mineral or organic acids with hydroxy or O-metal groups

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
C	ACYCLIC OR CARBOCYCLIC COMPOUNDS
41	Preparation of ethers; Preparation of compounds having groups, groups or groups
01	Preparation of ethers
16	by reaction of esters of mineral or organic acids with hydroxy or O-metal groups

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
C	ACYCLIC OR CARBOCYCLIC COMPOUNDS
41	Preparation of ethers; Preparation of compounds having groups, groups or groups
01	Preparation of ethers
16	by reaction of esters of mineral or organic acids with hydroxy or O-metal groups

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
C	ACYCLIC OR CARBOCYCLIC COMPOUNDS
43	Ethers; Compounds having groups, groups or groups
02	Ethers
20	having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
23	containing hydroxy or O-metal groups

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
C	ACYCLIC OR CARBOCYCLIC COMPOUNDS
41	Preparation of ethers; Preparation of compounds having groups, groups or groups
01	Preparation of ethers
16	by reaction of esters of mineral or organic acids with hydroxy or O-metal groups

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1. WO2016108172 - PROCESS FOR THE PREPARATION OF OSPEMIFENE AND FISPEMIFENE