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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
    1.
    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
    5.
    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。

    Pyrrolidine compounds and process of preparing
    6.
    再颁专利
    Pyrrolidine compounds and process of preparing 有权
    吡咯烷化合物及其制备方法

    公开(公告)号：USRE36607E

    公开(公告)日：2000-03-07

    申请号：US276220

    申请日：1999-03-25

    申请人： Joachim Mittendorf ,  Peter Fey ,  Bodo Junge ,  Johannes Kaulen ,  Kai van Laak ,  Heinrich Meier ,  Rudolf Schohe-Loop

    发明人： Joachim Mittendorf ,  Peter Fey ,  Bodo Junge ,  Johannes Kaulen ,  Kai van Laak ,  Heinrich Meier ,  Rudolf Schohe-Loop

    IPC分类号： A61K31/4412 ,  A61P25/28 ,  C07D207/40 ,  C07D207/416 ,  C07D211/80 ,  C07D211/90 ,  C07D401/02 ,  C07D401/06 ,  C07D401/12 ,  C07D521/00

    CPC分类号： C07D207/416 ,  C07D211/90 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/12

    摘要： This invention relates to benzolididene compounds of the formula ##STR1## in which R.sup.2 represents the radical ##STR2## in which R.sup.4 and R.sup.5 are identical or different and denote halogen, cyano, ethinyl, trifluoromethoxy, methylthio, nitro, trifluoromethyl or straight-chain or branched alkyl, alkenyl, alkinyl or alkoxy having up to 4 carbon atoms, and one of the substituents optionally represents hydrogen,or a salt thereof.[...]..Iadd., andA represents hydrogen or straight-chain or branched alkyl having up to 8 carbon atoms, or represents phenyl or benzyl which are optionally substituted one to three times by identical or different substituents from the series consisting of hydroxyl, nitro, halogen, cyano, carboxyl, trifluoromethyl, trifluoromethoxy, straight-chain or branched alkoxy having up to 6 carbon atoms or by a group of the formula --NR.sup.6 R.sup.7 or --SO.sub.2 R.sup.8, in whichR.sup.6 and R.sup.7 are identical or different and denote hydrogen, phenyl or straight-chain or branched alkyl having up to 5 carbon atomsandR.sup.8 denotes straight-chain or branched alkyl having up to 4 carbon atoms or phenyl. .Iaddend.

    摘要翻译： 本发明涉及下式的苯偶姻化合物，其中R 2表示其中R 4和R 5相同或不同并且表示卤素，氰基，乙炔基，三氟甲氧基，甲硫基，硝基，三氟甲基或直链或支链烷基，烯基，炔基 或具有至多4个碳原子的烷氧基，其中一个取代基任选代表氢或其盐[和]，A表示氢或具有至多8个碳原子的直链或支链烷基，或表示苯基或苄基， 任选地被羟基，硝基，卤素，氰基，羧基，三氟甲基，三氟甲氧基，具有至多6个碳原子的直链或支链烷氧基或通过下式的基团取代的相同或不同的取代基取代一至三次： -NR6R7或-SO2R8，其中R6和R7相同或不同，表示氢，苯基或具有至多5个碳原子的直链或支链烷基，R8表示直链 具有至多4个碳原子的直链或支链烷基或苯基。

    Method for producing N-methyl-N′-nitroguanidine
    8.
    发明授权
    Method for producing N-methyl-N′-nitroguanidine 有权
    制备N-甲基-N'-硝基胍的方法

    公开(公告)号：US06720451B2

    公开(公告)日：2004-04-13

    申请号：US10169842

    申请日：2002-07-09

    申请人： Kai van Laak ,  Wolfram Sirges

    发明人： Kai van Laak ,  Wolfram Sirges

    IPC分类号： C07C29100

    CPC分类号： C07C277/08 ,  C07C279/36

    摘要： The present invention relates to a novel process for the preparation of N-methyl-N′-nitroguanidine by reacting nitroguanidine with aqueous methylamine solution buffered by the addition of inorganic or organic acids.

    摘要翻译： 本发明涉及通过硝基胍与加入无机或有机酸缓冲的甲胺溶液反应制备N-甲基-N'-硝基胍的新方法。