Ring substituted pyrazino-isoquinoline derivatives and their preparation
    3.
    发明授权
    Ring substituted pyrazino-isoquinoline derivatives and their preparation 失效
    环取代的吡嗪异喹啉衍生物及其制备方法

    公开(公告)号:US4120961A

    公开(公告)日:1978-10-17

    申请号:US817467

    申请日:1977-07-20

    CPC分类号: C07D217/14

    摘要: Isoquinolines of the formula ##STR1## wherein R.sup.1 is H, OH, alkyl; R.sup.2 is H, or an unsubstituted or substituted carbonyl, carbonyloxy or thiocarbonyl group; R.sup.3 is H, alkyl or hydroxy alkyl; R.sup.4 is H, alkyl or phenyl; R.sup.5 is O, H,H or H and alkyl, phenyl, halo or hydroxy; R.sup.6 and R.sup.7 are optional substituents; and R.sup.8 is H or alkyl, R.sup.2 being a thiocarbonyl or carbonyloxy group when R.sup.1 and R.sup.3 to R.sup.8 are H and X is O; and their physiologically acceptable salts, are antihelmintics, especially against cestodes and trematodes; some also possessing CNS activity, e.g., psychotropic and blood pressure regulating activity.

    摘要翻译: 其中R 1是H,OH,烷基; R2是H或未取代或取代的羰基,羰基氧基或硫代羰基; R3是H,烷基或羟基烷基; R4是H,烷基或苯基; R5是O,H,H或H,烷基,苯基,卤素或羟基; R6和R7是任选的取代基; 当R 1和R 3至R 8为H且X为O时,R 8为H或烷基,R 2为硫代羰基或羰基氧基; 和它们的生理学上可接受的盐,是抗炎药,特别是针对绦虫和吸虫; 一些还具有CNS活性,例如精神病和血压调节活性。

    Pyrazinoisoquinolines as anthelmintic agents
    4.
    发明授权
    Pyrazinoisoquinolines as anthelmintic agents 失效
    吡嗪异喹啉作为驱肠剂

    公开(公告)号:US3993760A

    公开(公告)日:1976-11-23

    申请号:US481792

    申请日:1974-06-21

    CPC分类号: C07D471/04 C07D217/14

    摘要: (-)-2-Benzoyl-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline is prepared by benzoylation of (-)-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline, or cyclization of a compound of the formula ##SPC1##Wherein X is F, Cl, Br, I or O-tosyl and which has the optical configuration of the final product, or cyclization of a compound of the formula ##SPC2## wherein Y is OH, alkoxy, F, Cl, Br or I under HY-removing reaction conditions and which has the optical configuration of the final product, which is an anthelmintic.

    摘要翻译: ( - ) - 2-苯甲酰基-4-氧代-1,2,3,6,7,11b-六氢-4H-吡嗪并[2,1-a]异喹啉线是通过( - ) - 4-氧代 -1,2,3,6,7,11b-六氢-4H-吡嗪并[2,1-a]异喹啉,或式WHEREIN X的化合物与F,Cl,Br,I或O-甲苯磺酰基和 其具有最终产物的光学构型,或在HY-去除反应条件下环化下式化合物其中Y是OH,烷氧基,F,Cl,Br或I,并且具有最终产物的光学构型,其中 是一个驱魔。

    2-Acyl-4-oxo-pyrazino-isoquinoline derivatives and process for the
preparation thereof
    7.
    发明授权
    2-Acyl-4-oxo-pyrazino-isoquinoline derivatives and process for the preparation thereof 失效
    2-乙酰-4-氧代 - 吡咯并 - 异喹啉衍生物及其制备方法

    公开(公告)号:US4113867A

    公开(公告)日:1978-09-12

    申请号:US742132

    申请日:1976-11-15

    CPC分类号: C07D217/14

    摘要: 2-Acyl-4-oxo-hexahydro-4H-pyrazino[2,1-a]isoquinoline derivatives of the formula ##STR1## wherein COR is the acyl radical of an up to 26 carbon atom acid and their physiologically acceptable acid addition and quaternary ammonium salts, are anthelmintics and can be produced by reacting 4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline with an acid or a reactive functional derivative thereof.

    摘要翻译: 具有式“IMAGE”的2-酰基-4-氧代 - 六氢-4H-吡嗪并[2,1-a]异喹啉衍生物,其中COR是至多26个碳原子的酰基和它们的生理上可接受的酸加成和季 铵盐是驱虫剂,可以通过使4-氧代-1,2,3,6,7,11b-六氢-4H-吡嗪并[2,1-a]异喹啉与酸或其反应性官能衍生物 。

    2-Acyl-4-oxo-pyrazino-isoquinoline derivatives and process for the
preparation thereof
    8.
    发明授权
    2-Acyl-4-oxo-pyrazino-isoquinoline derivatives and process for the preparation thereof 失效
    2-酰基-4-氧代 - 吡嗪并 - 异喹啉衍生物及其制备方法

    公开(公告)号:US4196291A

    公开(公告)日:1980-04-01

    申请号:US970302

    申请日:1978-12-18

    IPC分类号: C07D217/14 C07D471/04

    CPC分类号: C07D217/14

    摘要: 2-Acyl-4-oxo-hexahydro-4H-pyrazino[2,1-a]isoquinoline derivatives of the formula ##STR1## wherein COR is the acyl radical of an up to 26 carbon atom acid and their physiologically acceptable acid addition and quaternary ammonium salts, are anthelmintics and can be produced by reacting 4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline with an acid or a reactive functional derivative thereof. This is a division, or application Ser. No. 742,133, filed on Nov. 15, 1976, which in turn is a divisional of Ser. No. 533,467, filed on Dec. 16, 1974, now U.S. Pat. No. 4,001,411.

    摘要翻译: 具有式“IMAGE”的2-酰基-4-氧代 - 六氢-4H-吡嗪并[2,1-a]异喹啉衍生物,其中COR是至多26个碳原子的酰基和它们的生理上可接受的酸加成和季 铵盐是驱肠虫剂,可以通过使4-氧代-1,2,3,6,7,11b-六氢-4H-吡嗪并[2,1-a]异喹啉与酸或其反应性官能衍生物反应来制备。 这是一个部门或应用程序 1976年11月15日提交的第742,133号,反过来是Ser。 1974年12月16日提交的美国专利533,467号。 第4,001,411号。