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    Process for the preparation of hydroxyamino-eburnane derivatives and octahydroindoloquinolizine intermediates
    1.
    发明授权
    Process for the preparation of hydroxyamino-eburnane derivatives and octahydroindoloquinolizine intermediates 失效
    羟基氨基 - 伊本烷衍生物和八氢吲哚喹啉中间体的制备方法

    公开(公告)号：US4345082A

    公开(公告)日：1982-08-17

    申请号：US154329

    申请日：1980-05-29

    申请人： Csaba Szantay ,  Lajos Szabo ,  Gyorgy Kalaus ,  Janos Sapi ,  Lajos Dancsi ,  Tibor Keve ,  Maria Gazdac

    发明人： Csaba Szantay ,  Lajos Szabo ,  Gyorgy Kalaus ,  Janos Sapi ,  Lajos Dancsi ,  Tibor Keve ,  Maria Gazdac

    IPC分类号： C07D459/00 ,  A61K31/435 ,  A61K31/4375 ,  A61K31/475 ,  A61P9/08 ,  C07D461/00 ,  C07D471/14 ,  C07D455/00

    CPC分类号： C07D471/14 ,  C07D461/00 ,  Y10S514/929

    摘要： The invention relates to new hydroxyamino-eburnane derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each stand for a C.sub.1-6 alkyl group, as well as to pharmaceutically acceptable acid addition salts and optically active isomers of these compounds.These new compounds can be applied as peripheral vasodilatating agents or can be converted into other compounds, e.g. vincamine and apovincamine derivatives of valuable therapeutical effects.The compounds of the general formula (I) are prepared according to the invention by reacting a hexahydro-indoloquinolisinium derivative of the general formula (II), ##STR2## wherein R.sup.2 is as defined above and X stands for an acid residue, with a methylenemalonic acid diester derivative of the general formula (III), ##STR3## wherein R.sup.1 is as defined above, subjecting the resulting product to catalytic hydrogenation, treating the resulting product with an alkali, and reacting the resulting octahydroindoloquinolisine monoester derivative with a nitrosating agent in an acidic medium.

    摘要翻译： 本发明涉及通式（I）的新型羟基氨基 - 伊本烷衍生物，其中R1和R2各自表示C1-6烷基，以及药学上可接受的酸加成盐和旋光异构体 的这些化合物。 这些新化合物可以作为外周血管舒张剂使用，也可以转化为其它化合物，例如 长春胺和氨基丁胺衍生物具有宝贵的疗效。 通式（I）的化合物根据本发明通过使通式（II）的六氢 - 吲哚并喹啉鎓衍生物，其中R 2如上定义，X​​代表酸残基， 与通式（III）的亚甲基丙二酸二酯衍生物，其中R 1如上定义，使所得产物进行催化氢化，用碱处理所得产物，并使所得八氢二吲哚并喹啉酮单酯衍生物 在酸性介质中使用亚硝化剂。

    Hexahydroindoloquinolizinium and octahydroindoloquinolizine esters, and method of increasing blood flow in an animal with hydroxyamino-eburnane derivatives
    2.
    发明授权
    Hexahydroindoloquinolizinium and octahydroindoloquinolizine esters, and method of increasing blood flow in an animal with hydroxyamino-eburnane derivatives 失效
    六氢吲哚喹啉鎓和八氢二吲哚喹啉酯，以及用羟基氨基 - 伊本恩衍生物增加动物血流量的方法

    公开(公告)号：US4446139A

    公开(公告)日：1984-05-01

    申请号：US351506

    申请日：1982-02-23

    申请人： Csaba Szantay ,  Lajos Szbao ,  Gyorgy Kalaus ,  Janos Sapi ,  Lajos Dancsi ,  Tibor Keve

    发明人： Csaba Szantay ,  Lajos Szbao ,  Gyorgy Kalaus ,  Janos Sapi ,  Lajos Dancsi ,  Tibor Keve

    IPC分类号： C07D461/00 ,  C07D471/14 ,  A61K31/435 ,  C07D455/00

    CPC分类号： C07D471/14 ,  C07D461/00

    摘要： The invention relates to new hydroxyamino-eburnane derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each stand for a C.sub.1-6 alkyl group, as well as to pharmaceutically acceptable acid addition salts and optically active isomers of these compounds.These new compounds can be applied as peripheral vasodilatating agents or can be converted into other compounds, e.g. vincamine and apovincamine derivatives, of valuable therapeutical effects.The compounds of the general formula (I) are prepared according to the invention by reacting a hexahydro-indoloquinolisinium derivative of the general formula (II), ##STR2## wherein R.sup.2 is as defined above and X stands for an acid residue, with a methylenemalonic acid diester derivative of the general formula (III), ##STR3## wherein R.sup.1 is as defined above, subjecting the resulting product to catalytic hydrogenation, treating the resulting product with an alkali, and reacting the resulting octahydroindoloquinolisine monoester derivative with a nitrosating agent in an acidic medium.

    摘要翻译： 本发明涉及通式（I）的新型羟基氨基 - 伊本烷衍生物，其中R1和R2各自表示C1-6烷基，以及药学上可接受的酸加成盐和旋光异构体 的这些化合物。 这些新化合物可以作为外周血管舒张剂使用，也可以转化为其它化合物，例如 长春胺和氨肽素衍生物，具有宝贵的疗效。 通式（I）的化合物根据本发明通过使通式（II）的六氢 - 吲哚并喹啉鎓衍生物，其中R 2如上定义，X​​代表酸残基， 与通式（III）的亚甲基丙二酸二酯衍生物，其中R1如上所定义，使所得产物进行催化氢化，用碱处理所得产物，并使所得八氢二吲哚并喹啉酮单酯衍生物 在酸性介质中使用亚硝化剂。

    Process for the preparation of halovincamone derivatives
    3.
    发明授权
    Process for the preparation of halovincamone derivatives 失效
    制备Halovincone酮衍生物的方法

    公开(公告)号：US4356305A

    公开(公告)日：1982-10-26

    申请号：US175384

    申请日：1980-08-05

    申请人： Csaba Szantay ,  Lajos Szabo ,  Gyorgy Kalaus ,  Lajos Dancsi ,  Tibor Keve ,  Ferenc Drexler

    发明人： Csaba Szantay ,  Lajos Szabo ,  Gyorgy Kalaus ,  Lajos Dancsi ,  Tibor Keve ,  Ferenc Drexler

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

    CPC分类号： C07D461/00

    摘要： The invention relates to new halovincamone derivatives of the general formula (I), ##STR1## wherein R is a C.sub.1-6 alkyl group and X is halogen, and pharmaceutically acceptable acid addition salts and optically active isomers thereof. These compounds possess valuable vasodilating effect, and can be applied to advantage in the therapy.The new compounds defined above are prepared according to the invention so that a single epimer or an epimeric mixture of a racemic or optically active halogenated 14-oxo-15-hydroxy-E-homoeburnane derivative of the general formula (II), ##STR2## wherein R and X are as defined above, or an acid addition salt thereof is treated with an oxidizing agent, and, if desired, the resulting compound of the general formula (I) is converted into its pharmaceutically acceptable acid addition salt and/or resolved.

    摘要翻译： 本发明涉及通式（I）的新的Halovincone酮衍生物，其中R是C 1-6烷基，X是卤素的化合物及其药学上可接受的酸加成盐和旋光异构体。 这些化合物具有有价值的血管扩张作用，可用于治疗中的优势。 根据本发明制备上述新化合物，使得通式（II）的外消旋或光学活性的卤代14-氧代-15-羟基-E-高拜尔班恩衍生物的单个差向异构体或差向异构体混合物 （II）其中R和X如上所定义，或其酸加成盐用氧化剂处理，如果需要，将所得的通式（I）化合物转化为其药学上可接受的酸加成盐和 /或解决。

    Process for the preparation of apovincaminic acid ester derivatives
    5.
    发明授权
    Process for the preparation of apovincaminic acid ester derivatives 失效
    氨基丁酸酯衍生物的制备方法

    公开(公告)号：US4400514A

    公开(公告)日：1983-08-23

    申请号：US209265

    申请日：1980-11-21

    申请人： Csaba Szantay ,  Lajos Szabo ,  Gyorgy Kalaus ,  Lajos Dancsi ,  Tibor Keve ,  Ferenc Drexler ,  Krisztina Mihalyfi

    发明人： Csaba Szantay ,  Lajos Szabo ,  Gyorgy Kalaus ,  Lajos Dancsi ,  Tibor Keve ,  Ferenc Drexler ,  Krisztina Mihalyfi

    IPC分类号： B01J23/00 ,  C07B61/00 ,  C07D461/00 ,  C07D471/22

    CPC分类号： C07D461/00

    摘要： The invention concerns a new process for the preparation of apovincaminic acid ester derivatives of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 independently represent an alkyl group having 1 to 6 carbon atoms,and pharmaceutically acceptable salts thereof.According to the invention the apovincaminic acid ester derivatives of the general formula (I) are prepared by reacting the corresponding 9- and/or 10- and/or 11-halo-14-oxo-15-hydroxyimino-E-homo-eburnane derivatives with an alkanol of the general formula R.sup.1 --OH, wherein R.sup.1 is as defined above, and with a dehydrating concentrated acid, and subsequently reducing the 9- and/or 10- and/or 11-halo-apovincaminic acid esters obtained, selectively on the aromatic ring. Alternatively, the 9- and/or 10- and/or 11-halo-apovincaminic acid esters can also be used as starting materials. The invention includes the preparation of racemic and optically active apovincaminic acid ester derivatives and of their pharmaceutically acceptable salts, as well.

    摘要翻译： 本发明涉及一种制备通式（I）的氨基苯甲酸酯衍生物的新方法，其中R1和R2独立地表示具有1至6个碳原子的烷基，及其药学上可接受的盐。 根据本发明，通式（I）的氨基亚氨酸酯衍生物通过相应的9-和/或10-和/或11-卤代-14-氧代-15-羟基亚氨基-E-高 - 伊本恩衍生物 与通式R 1 -OH的烷醇，其中R 1如上定义，并与脱水浓酸反应，然后选择性地将所得的9-和/或10-和/或10-卤代 - 氨基丁酸酯还原 芳香环。 或者，9-和/或10-和/或11-卤代 - 氨基丁酸酯也可以用作原料。 本发明还包括外消旋和光学活性氨肽酸酯衍生物及其药学上可接受的盐的制备。

    10-halo-E-homoeburnane derivatives, a process for the preparation thereof, a process for the use thereof as vasodilators, and vasodilating compositions thereof
    6.
    发明授权
    10-halo-E-homoeburnane derivatives, a process for the preparation thereof, a process for the use thereof as vasodilators, and vasodilating compositions thereof 失效
    10-卤代-E-高聚乙二醇衍生物，其制备方法，其用作血管扩张剂的方法及其血管舒张组合物

    公开(公告)号：US4285950A

    公开(公告)日：1981-08-25

    申请号：US175383

    申请日：1980-08-05

    申请人： Csaba Szantay ,  Lajos Szabo ,  Gyorgy Kalaus ,  Lajos Dancsi ,  Tibor Keve ,  Ferenc Drexler

    发明人： Csaba Szantay ,  Lajos Szabo ,  Gyorgy Kalaus ,  Lajos Dancsi ,  Tibor Keve ,  Ferenc Drexler

    IPC分类号： A61K31/55 ,  A61P9/08 ,  A61P9/10 ,  C07D461/00 ,  C07D471/22 ,  A61K31/395

    CPC分类号： C07D471/22 ,  Y10S514/929

    摘要： The invention relates to new 10-halo-E-homoeburnane derivatives of the general formula (I), ##STR1## wherein R.sup.2 is a C.sub.1-6 alkyl group and X is halogen, and epimers, optically active derivatives and pharmaceutically acceptable acid addition salts thereof. These substances exert vasodilating effects and can be applied to advantage in the therapy.The new compounds are prepared so that a racemic or optically active 9-halo-octahydroindoloquinolisine derivative of the general formula (II), ##STR2## wherein R.sup.2 and X are as defined above and R.sup.1 is a C.sub.1-6 alkyl group, or an acid addition salt thereof is treated with a strong base, and, if desired, the 15-epimers of the resulting compound having the general formula (I) are separated from each other, and/or, if desired, the resulting substance is converted into its pharmaceutically acceptable acid addition salt and/or resolved.

    摘要翻译： 本发明涉及通式（I）的新的10-卤代 - 均 - 甲硼烷衍生物，其中R2是C1-6烷基且X是卤素的差向异构体，光学活性衍生物和药学上可接受的衍生物 其酸加成盐。 这些物质发挥血管扩张作用，可用于治疗中的优势。 制备新化合物，使得通式（II）的外消旋或光学活性的9-卤代 - 八氢吲哚-2-醇衍生物，其中R 2和X如上所定义，R 1是C 1-6烷基， 或其酸加成盐用强碱处理，如果需要，所得化合物的具有通式（I）的15-差向异构体彼此分离，和/或如果需要，所得物质为 转化成其药学上可接受的酸加成盐和/或分解。

    Process for the preparation of 15-hydroxyimino-E-homoeburnane and intermediates therefor
    8.
    发明授权
    Process for the preparation of 15-hydroxyimino-E-homoeburnane and intermediates therefor 失效
    制备15-羟基亚氨基-E-高聚乙二醇的方法及其中间体

    公开(公告)号：US4314939A

    公开(公告)日：1982-02-09

    申请号：US168560

    申请日：1980-07-14

    申请人： Csaba Szantay ,  Lajos Szabo ,  Gyorgy Kalaus ,  Lajos Dancsi ,  Tibor Keve ,  Ferenc Drexler

    发明人： Csaba Szantay ,  Lajos Szabo ,  Gyorgy Kalaus ,  Lajos Dancsi ,  Tibor Keve ,  Ferenc Drexler

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

    CPC分类号： C07D471/22

    摘要： A process for the preparation of 15-hydroxyimino-E-homoeburnane derivatives of the formula (I), ##STR1## wherein X.sup.1 stands for hydrogen or halogen andR is a C.sub.1-6 alkyl group,or acid addition salts and optically active derivatives thereof. These compounds are valuable intermediates of the synthesis of compounds with outstanding biological effects. According to the invention a racemic or optically active 15-hydroxy-E-homoeburnane derivative of the formula (II), ##STR2## is treated, optionally after separating the 15-epimers and/or resolution, with a halogenating agent. The resulting 15-halo-E-homoeburnane derivative of the formula (III), ##STR3## wherein X.sup.2 stands for halogen, is reacted, optionally after separating the 15 epimers and/or resolution, with an alkali nitrite in the presence of an acid, and, if desired, the resulting 15-hydroxyimino-E-homoeburnane derivative of the formula (I) is converted into its acid addition salt and/or resolved. The compounds of the formula (III) formed as intermediates in the above process are new and biologically active.

    摘要翻译： 制备式（I）的XV-羟基亚氨基-E-高硼烷衍生物的方法，其中X1代表氢或卤素，R是C1-6烷基，或酸加成盐和光学 其活性衍生物。 这些化合物是合成具有突出生物学作用的化合物的有价值的中间体。 根据本发明，任选地在用卤化剂分离15-差向异构体和/或拆分之后处理式（II）的外消旋或光学活性的15-羟基-E-高硼烷衍生物。 所得到的式（III）的15-卤代-E-高硼烷衍生物，其中X 2代表卤素，其中任选地在存在15个差向异构体和/或拆分之前用碱金属亚硝酸盐反应， 的酸，如果需要，将所得的式（I）的15-羟基亚氨基-E-高硼烷衍生物转化为其酸加成盐和/或分解。 在上述方法中形成作为中间体的式（III）化合物是新的和生物活性的。

    Process for the preparation of 11-bromo-vincaminic acid ester derivatives and their use in protecting animals against cerebral hypoxy
    9.
    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。