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    Process for the preparation of optically active 2-aryl-alkanoic acids, especially 2-aryl-propionic acids
    9.
    发明授权
    Process for the preparation of optically active 2-aryl-alkanoic acids, especially 2-aryl-propionic acids 失效
    用于制备光学活性2-芳基 - 链烷酸，特别是2-芳基 - 丙酸的方法

    公开(公告)号：US5266723A

    公开(公告)日：1993-11-30

    申请号：US486979

    申请日：1990-02-27

    申请人： Samir B. Hanna ,  Bernd Schneider ,  Henrich H. Paradies

    发明人： Samir B. Hanna ,  Bernd Schneider ,  Henrich H. Paradies

    IPC分类号： A61K9/14 ,  A61K9/48 ,  C07C51/15 ,  C07C57/30 ,  C07L59/48 ,  C07L63/36

    CPC分类号： C07C57/30 ,  A61K9/146 ,  A61K9/4858 ,  C07C51/15 ,  Y02P20/582

    摘要： A chemical process is disclosed for the preparation of a pharmaceutically active compound in an enantiomeric form either (R) or (S) of the structure ##STR1## and a suitable pharmaceutical salt, e.g. alkali or earth metal, D-glucamine or D-ribamine, where R.sub.1 represents an optionally substituted aryl group same as phenyl or naphthyl group, optionally including a heterocyclic ring system, which is optionally substituted, or represents a hetero-aromatic ring system optionally containing in addition to carbon atoms one or more atoms selected from the group consisting of nitrogen and oxygen; the enantiomeric R or S-compounds of (I) are obtained from a suitable ketone (II) by reduction with an LiAlH.sub.4.sup.- "chiraldid-complex" to the corresponding S- or R-alcohol, following chlorination with retention of configuration, and producing a steriochemical pure R or S magnesium organic compound by subsequent carbonation with carbon dioxide in the presence of a ligand by keeping the stereochemical configuration R or S at 98% enantiomeric excess at least including high yields, and if desired converting compounds (I) into a pharmaceutically acceptable salt or ester thereof. Especially pharmaceutically complexes with D-glucamine and D-ribamine in a stoichiometric ratio of 1:1, including salts comprised of N-cationic detergents with 2-(S)-aryl-alkanoic acids.

    摘要翻译： 公开了用于制备对映体形式的药学活性化合物的化学方法（R）或（S）结构（I）图像（II）和适合的药物盐，例如， 碱金属或土壤金属，D-葡萄糖胺或D-核糖胺，其中R 1表示任选取代的与苯基或萘基相同的芳基，任选地包括任选被取代的杂环体系，或表示任选含有 除了碳原子之外还有一个或多个选自氮和氧的原子; （I）的对映异构体R或S-化合物通过在保持配置的氯化之后用LiAlH 4 - “手性偶联物”还原成相应的S-或R-醇从合适的酮（II）获得，并产生 通过在配体存在下通过保持立体化学构型R或S至少包括高产率的98％对映异构体过量，随后与二氧化碳碳酸化而产生无机化学纯的R或S镁有机化合物，如果需要，将化合物（I）转化为 其药学上可接受的盐或酯。 特别是与D-葡萄糖胺和D-核糖胺以化学计量比为1:1的药物复合物，包括由N-阳离子去污剂与2-（S） - 芳基 - 链烷酸组成的盐。