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    Process for the preparation of 11-bromo-vincaminic acid ester derivatives and their use in protecting animals against cerebral hypoxy
    8.
    发明授权
    Process for the preparation of 11-bromo-vincaminic acid ester derivatives and their use in protecting animals against cerebral hypoxy 失效
    制备11-溴 - 长春胺酸酯衍生物的方法及其在保护动物免受脑缺氧的作用

    公开(公告)号：US4283401A

    公开(公告)日：1981-08-11

    申请号：US56647

    申请日：1979-07-11

    申请人： Csaba Szantay ,  Lajos Szabo ,  Gyorgy Kalaus ,  Lajos Dancsi ,  Tibor Keve ,  Egon Karpati ,  Laszlo Szporny

    发明人： Csaba Szantay ,  Lajos Szabo ,  Gyorgy Kalaus ,  Lajos Dancsi ,  Tibor Keve ,  Egon Karpati ,  Laszlo Szporny

    IPC分类号： C07D461/00 ,  C07D471/22 ,  A61K31/55 ,  C07D459/00

    CPC分类号： C07D461/00

    摘要： A novel process for preparing 11-bromo-vincaminic acid esters of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each stand independently from each other for a C.sub.1-6 alkyl group, comprising the steps of treating a 1-alkyl-1-alkoxycarbonylethyl-octahydroindolo-quinolisine of the general formula ##STR2## wherein R.sup.2 is as defined above and R.sup.3 stands for a C.sub.1-6 alkyl group, with a brominating agent and treating the resulting isomeric mixture of the bromo-derivatives with an alkaline agent or treating the corresponding 14-oxo-E-homo-eburnane being unsubstituted in ring A with a brominating agent and nitrosating the resulting 11-bromo-14-oxo-E-homo-eburnane of the general formula ##STR3## wherein R.sup.2 is as defined above, then subjecting the resulting 11-bromo-14-oxo-15-hydroxyimino-E-homoeburnanes to deoxyimination and treating the 14,15-dioxo-derivatives obtained with a base in an alcohol of the general formula R.sup.1 OH, wherein R.sup.1 is as defined above.All the intermediate products are novel and exhibit a therapeutical protecting effect against cerebral hypoxy.

    摘要翻译： 一种用于制备通式为“IMAGE”的11-溴 - 长春胺酸酯的新方法，其中R 1和R 2各自独立地为C 1-6烷基独立地包括如下步骤：将1-烷基-1-烷氧基羰基乙基 其中R 2如上所定义，R 3表示C 1-6烷基，与溴化剂反应，并用碱处理所得到的溴代衍生物的异构体混合物或处理 环A中未取代的相应的14-氧代-E-均 - 异丁苯与溴化剂并亚硝化所得的通式为“IMAGE”的11-溴-14-氧代-E-均 - 胡烷，其中R2如上定义， 然后将所得的11-溴代-14-氧代-15-羟基亚氨基-E-高硼烷进行脱氧亚胺化处理，并用在通式为R 1 OH的醇中用碱获得的14,15-二氧代衍生物进行脱氧，其中R1如上定义 。 所有的中间产物都是新颖的，并且对脑缺氧具有治疗保护作用。