US20170342007 Process for the preparation of ospemifene and fispemifene

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United States of America

Application Number 15539695

Application Date 28.12.2015

Publication Number 20170342007

Publication Date 30.11.2017

Grant Number 09975832

Grant Date 22.05.2018

Publication Kind B2

IPC

CPC

Applicants OLON S.P.A.

Inventors Tania Cristiano
Marco Alpegiani

Agents Silvia Salvadori, P.C.
Silvia Salvadori

Priority Data MI2014A2267 29.12.2014 IT

Title

(EN) Process for the preparation of ospemifene and fispemifene

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.

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

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. US20170342007 - Process for the preparation of ospemifene and fispemifene