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    Nintrovincaminic acid derivatives having pharmaceutical utility
    5.
    发明授权
    Nintrovincaminic acid derivatives having pharmaceutical utility 失效
    具有药用效用的新一代氨基酸衍生物

    公开(公告)号：US4810709A

    公开(公告)日：1989-03-07

    申请号：US105959

    申请日：1987-10-07

    申请人： Andras Vedres ,  Csaba Szantay ,  Istvan Moldvai ,  Bela Stefko ,  Dora Groo ,  Egon Karpati ,  Bela Kiss ,  Eva Palosi ,  Miklos Riesz ,  Zsolt Szombathelyi ,  Laszlo Szporny ,  Maria Zajer nee Balazs

    发明人： Andras Vedres ,  Csaba Szantay ,  Istvan Moldvai ,  Bela Stefko ,  Dora Groo ,  Egon Karpati ,  Bela Kiss ,  Eva Palosi ,  Miklos Riesz ,  Zsolt Szombathelyi ,  Laszlo Szporny ,  Maria Zajer nee Balazs

    IPC分类号： A61K31/435 ,  A61P9/00 ,  A61P9/08 ,  A61P25/08 ,  C07D461/00 ,  A61K31/475

    CPC分类号： C07D461/00

    摘要： The invention relates to a new process for preparing novel racemic and optically active 9- or 11-nitroapovincaminic acid derivatives of the general formula (I) ##STR1## wherein R stands for a --CO--X group, wherein X means a halogen atom; orfor a --CO--OR.sup.1 group, wherein R.sup.1 means an optionally mono- or polysubstituted C.sub.1-10 aliphatic group, a C.sub.3-8 alicyclic group or an aromatic C.sub.6-14 hydrocarbyl group; orfor a --CO--NR.sup.2 R.sup.3 group, wherein R.sup.2 and R.sup.3 are the same or different and stand for a hydrogen atom or a C.sub.1-8 alkyl group optionally forming a saturated heterocycle together with the adjacent nitrogen atom and optionally with one or more further nitrogen atoms or other heteroatoms, and R.sup.3 may also represent an amino group when R.sup.2 stands for a hydrogen atom; orfor a cyano group,as well as their salts and pharmaceutical preparations containing these compounds. Furthermore the invention relates to a process for preparing these compounds and preparations.The racemic and optically active substances of the general formula (I) as well as their pharmaceutically acceptable acid addition and quaternary salts have valuable therapeutic properties, namely vasodilating, spasmolytic, antihypoxic and anticonvulsive effects.

    摘要翻译： 本发明涉及制备通式（I）的新型外消旋和光学活性的9-或11-硝基
    氨基嘌呤酸衍生物的新方法，其中R代表-CO-X基团，其中X表示 卤素原子; 或-CO-OR 1基团，其中R 1表示任选的单取代或多取代的C 1-10脂族基团，C 3-8脂环族基团或芳族C 6-14烃基; 或-CO-NR 2 R 3基团，其中R 2和R 3相同或不同，代表氢原子或任选地与相邻的氮原子一起形成饱和杂环的C 1-8烷基，并且任选地与一个或多个另外的氮 原子或其它杂原子，当R 2代表氢原子时，R 3也可以表示氨基; 或氰基，以及它们的含有这些化合物的盐和药物制剂。 此外，本发明涉及一种制备这些化合物和制剂的方法。 通式（I）的外消旋和光学活性物质及其药学上可接受的酸加成盐和季盐具有有价值的治疗性质，即血管舒张，解痉，抗缺氧和抗惊厥作用。

    Process for dehydration of condensation reaction mixtures obtained by azeotropic distillation
    10.
    发明授权
    Process for dehydration of condensation reaction mixtures obtained by azeotropic distillation 失效
    通过共沸蒸馏得到的缩合反应混合物的脱水方法

    公开(公告)号：US5137605A

    公开(公告)日：1992-08-11

    申请号：US598404

    申请日：1990-10-15

    申请人： Istvan Greiner ,  Jeno Szilbereky ,  Bela Stefko ,  Gyorgy Thaler

    发明人： Istvan Greiner ,  Jeno Szilbereky ,  Bela Stefko ,  Gyorgy Thaler

    IPC分类号： B01D3/36 ,  C07C41/58

    CPC分类号： C07C67/08 ,  B01D3/36 ,  C07C231/02 ,  C07C41/56 ,  C07C41/58 ,  C07C67/54

    摘要： A process for the dehydration of substances, mixtures, primarily condensation reaction mixtures, (e.g. direct esterification, direct acetal formation, direct ketal formation), performed by continuous azeotropic distillation with an organic solvent forming with water an azeotropic mixture of minimal boiling point and unable to mix with water, carried out in such a way that the distillate is cooled at least to the temperature, at which the condensate with the given water content or the organic phase of the condensate is just supersaturated with respect to water, and the organic phase of lower water content obtained in this way is recycled to the distilling boiler. The organic solvents used are e.g. benzene, toluene, 1,2-dichloroethane, chloroform, carbon tetrachloride.

    摘要翻译： 物质，混合物，主要是缩合反应混合物（例如直接酯化，直接缩醛形成，直接缩酮形成）的脱水方法是通过与水形成的有机溶剂进行连续共沸蒸馏，沸点最低的共沸混合物和无法 与水混合，使得馏出物至少冷却至具有给定水含量的冷凝物或冷凝物的有机相刚好相对于水过饱和的温度，并且有机相 以这种方式获得的较低含水量被再循环到蒸馏锅炉。 所使用的有机溶剂是例如 苯，甲苯，1,2-二氯乙烷，氯仿，四氯化碳。