EP 2566580 A1 20130313 - PROCESS FOR THE PREPARATION OF BIMOSIAMOSE
Title (en)
PROCESS FOR THE PREPARATION OF BIMOSIAMOSE
Title (de)
VERFAHREN ZUR HERSTELLUNG VON BIMOSIAMOSE
Title (fr)
PROCÉDÉ D'ÉLABORATION DE BIMOSIAMOSE
Publication
Application
Priority
- EP 10162276 A 20100507
- EP 2011057130 W 20110504
- EP 11720069 A 20110504
Abstract (en)
[origin: WO2011138365A1] A process for the preparation of 1,6-Bis-[3-(3-carboxymethylphenyl)-4-(2-a-D-mannopyranosyloxy)-phenyl] hexane (I) which comprises the steps of converting the compound (2'-Methoxy-biphenyl-3-yl)-acetic acid (A) into the (2'-Methoxy-biphenyl-3-yl)-acetic acid ethyl ester, which is reacted with adipoyl chloride to 1,4-Bis-[3-(3-carboethoxymethylphenyl)-4-methoxybenzoyl]-butane (B) which is catalytically reduced to 1,6-Bis-[3-(3-carboethoxy-methylphenyl)-4-methoxy- phenyl] -hexane (C), which is reacted with boron tribromide in a solvent to 1,6-Bis-[3-(3- carboethoxy-methylphenyl)-4-hydroxyphenyl]-hexane (D), which is reacted with a mannopyranosyl derivative to obtain 1,6-Bis-[3-(3-carboethoxy-methylphenyl)-4-(tetra-0- pivaloyl-a-D-mannopyranosyloxy)-phenyl]-hexane (E), which is reacted to form 1,6-Bis- [3-(3-carboxymethyl-phenyl)-4-(2-a-D-mannopyranosyloxy)-phenyl] hexane, which is re- crystallized, leads to the product (I) with high purity.
IPC 8 full level
A61P 11/00 (2006.01); C07H 15/203 (2006.01)
CPC (source: EP KR)
A61K 31/70 (2013.01 - KR); A61P 1/02 (2018.01 - EP); A61P 1/04 (2018.01 - EP); A61P 11/00 (2018.01 - EP); A61P 27/02 (2018.01 - EP); A61P 27/16 (2018.01 - EP); A61P 29/00 (2018.01 - EP); C07H 15/203 (2013.01 - EP KR); Y02P 20/55 (2015.11 - EP)
Designated contracting state (EPC)
AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
DOCDB simple family (publication)
WO 2011138365 A1 20111110; AU 2011249843 A1 20121129; CA 2798383 A1 20111110; CN 103002951 A 20130327; EP 2566580 A1 20130313; JP 2013525467 A 20130620; KR 20130056238 A 20130529; RU 2012152633 A 20140620
DOCDB simple family (application)
EP 2011057130 W 20110504; AU 2011249843 A 20110504; CA 2798383 A 20110504; CN 201180023098 A 20110504; EP 11720069 A 20110504; JP 2013508490 A 20110504; KR 20127029201 A 20110504; RU 2012152633 A 20110504