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    Process for the preparation of enantiomerically pure cycloalkano-indol -and azaindol -and pyrimido �1,2a! indolcarboxcyclic acids and their activated derivatives
    3.
    发明授权
    Process for the preparation of enantiomerically pure cycloalkano-indol -and azaindol -and pyrimido �1,2a! indolcarboxcyclic acids and their activated derivatives 失效
    制备对映异构纯的环烷基 - 吲哚 - 和氮杂吲哚和嘧啶并[1,2a]吲哚羧酸及其活化衍生物的方法

    公开(公告)号：US5952498A

    公开(公告)日：1999-09-14

    申请号：US829566

    申请日：1997-03-31

    申请人： Jan-Bernd Lenfers ,  Peter Fey ,  Paul Naab ,  Kai Van Laak

    发明人： Jan-Bernd Lenfers ,  Peter Fey ,  Paul Naab ,  Kai Van Laak

    IPC分类号： C07C69/612 ,  C07C69/616 ,  C07C69/65 ,  C07D471/04 ,  C07D487/04

    CPC分类号： C07D471/04 ,  C07C69/612 ,  C07C69/616 ,  C07C69/65 ,  C07D487/04

    摘要： The invention relates to a process and intermediates for the preparation of enantiomerically pure cycloalkanoindolecarboxylic acids and azaindolecarboxylic acids and pyrimido�1,2a!indolecarboxylic acids and their activated derivatives, characterized in that the tolyl acetic acid is first esterified with a chiral alcohol, then diastereoselective substitution at .alpha.-carbon atoms is carried out and this product is halogenated in the tolyl group and then reacted with appropriate cycloalkanoindoles, cycloalkanoazaindoles or pyrimido�1,2a!indoles. It is possible by this method to prepare specifically, in high purity, the enantiomerically pure carboxylic acids which are intermediates for valuable medicaments.

    摘要翻译： 本发明涉及制备对映体纯的环烷基吲哚羧酸和氮杂吲哚羧酸和嘧啶并[1,2a]吲哚羧酸及其活化衍生物的方法和中间体，其特征在于首先用手性醇酯化甲苯基乙酸，然后进行非对映选择性 在α-碳原子上进行取代，将该产物在甲苯基中卤化，然后与合适的环亚烷基吲哚，环烷基烷基偶氮或嘧啶并[1,2a]吲哚反应。 通过该方法可以高纯度地制备作为有价值药物的中间体的对映体纯的羧酸。

    Process for the preparation of enantiomerically pure cycloalkano-indol -and azaindol -and pyrimido [1,2A]indolcarbocyclic acids and their activated derivatives
    4.
    发明授权
    Process for the preparation of enantiomerically pure cycloalkano-indol -and azaindol -and pyrimido [1,2A]indolcarbocyclic acids and their activated derivatives 失效
    制备对映异构体纯的环烷基 - 吲哚 - 和氮杂吲哚和嘧啶并[1,2A]吲哚羧酸及其活化衍生物的方法

    公开(公告)号：US06774236B1

    公开(公告)日：2004-08-10

    申请号：US09307980

    申请日：1999-05-10

    申请人： Jan-Bernd Lenfers ,  Peter Fey ,  Paul Naab ,  Kai Van Laak

    发明人： Jan-Bernd Lenfers ,  Peter Fey ,  Paul Naab ,  Kai Van Laak

    IPC分类号： C07D47104

    CPC分类号： C07D471/04 ,  C07C69/612 ,  C07C69/616 ,  C07C69/65 ,  C07D487/04

    摘要： The invention relates to a process and intermediates for the preparation of enantiomerically pure cycloalkanoindolecarboxylic acids and azaindolecarboxylic acids and pyrimido[1,2a]indolecarboxylic acids and their activated derivatives, characterized in that the tolyl acetic acid is first esterified with a chiral alcohol, then diastereoselective substitution at &agr;-carbon atoms is carried out and this product is halogenated in the tolyl group and then reacted with appropriate cycloalkanoindoles, cycloalkanoazaindoles or pyrimido[1,2a]indoles. It is possible by this method to prepare specifically, in high purity, the enantiomerically pure carboxylic acids which are intermediates for valuable medicaments.

    摘要翻译： 本发明涉及制备对映体纯的环烷基吲哚羧酸和氮杂吲哚羧酸和嘧啶并[1,2a]吲哚羧酸及其活化衍生物的方法和中间体，其特征在于首先用手性醇酯化甲苯基乙酸，然后进行非对映选择性 在α-碳原子上进行取代，并将该产物在甲苯基中卤化，然后与适当的环亚烷基吲哚，环烷基烷基偶氮或嘧啶并[1,2a]吲哚反应。 通过该方法可以高纯度地制备作为有价值药物的中间体的对映体纯的羧酸。