发明名称 PROCESS FOR THE PREPARATION OF BIMOSIAMOSE
摘要 <p>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.</p>
申请公布号 WO2011138365(A1) 申请公布日期 2011.11.10
申请号 WO2011EP57130 申请日期 2011.05.04
申请人 REVOTAR BIOPHARMACEUTICALS AG;KRANICH, REMO;BOCK, DANIEL 发明人 KRANICH, REMO;BOCK, DANIEL
分类号 A61P11/00;C07H15/203 主分类号 A61P11/00
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