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    • 10. 发明申请
    • PROCESS FOR THE PREPARATION OF BIMOSIAMOSE
    • 制备双酚A的方法
    • WO2011138365A1
    • 2011-11-10
    • PCT/EP2011/057130
    • 2011-05-04
    • REVOTAR BIOPHARMACEUTICALS AGKRANICH, RemoBOCK, Daniel
    • KRANICH, RemoBOCK, Daniel
    • A61P11/00C07H15/203
    • C07H15/203
    • A process for the preparation of 1,6-Bis-[3-(3-carboxymethylphenyl)-4-(2-α-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-α-D-mannopyranosyloxy)-phenyl]-hexane (E), which is reacted to form 1,6-Bis- [3-(3-carboxymethyl-phenyl)-4-(2-α-D-mannopyranosyloxy)-phenyl] hexane, which is re- crystallized, leads to the product (I) with high purity.
    • 制备1,6-双 - [3-(3-羧甲基苯基)-4-(2-aD-甘露吡喃糖基氧基) - 苯基]己烷(I)的方法,其包括将化合物(2'-甲氧基 - 联苯-3-基) - 乙酸(A)加入到(2'-甲氧基 - 联苯-3-基) - 乙酸乙酯中,将其与己二酰氯与1,4-双[3-( (3-乙氧羰基甲基苯基)-4-甲氧基苯甲酰基]丁烷(B),其被催化还原成1,6-双 - [3-(3-乙酰氧基 - 甲基苯基)-4-甲氧基 - 苯基] - 己烷(C) 与三溴化硼在溶剂中与1,6-双 - [3-(3-乙酰氧基 - 甲基苯基)-4-羟基苯基] - 己烷(D)反应,其与甘草吡喃糖基衍生物反应,得到1,6-双 - [3-(3-乙酰氧基 - 甲基苯基)-4-(四-O-新戊酰基-DA-甘露吡喃糖基氧基) - 苯基] - 己烷(E),其反应形成1,6-双 - [3- 羧甲基 - 苯基)-4-(2-aD-甘露吡喃糖基氧基) - 苯基]己烷重结晶,得到高纯度的产物(I)。