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1. US20170342007 - Process for the preparation of ospemifene and fispemifene

Office
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
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
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 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.