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    Process for the preparation of 9-hydrazono-6,7,8,9-tetrahydro-4H-pyro[1,2-a]pyrimidine-4-one compounds, the salts and hydrates thereof
    11.
    发明授权
    Process for the preparation of 9-hydrazono-6,7,8,9-tetrahydro-4H-pyro[1,2-a]pyrimidine-4-one compounds, the salts and hydrates thereof 失效
    制备9-亚肼基-6,7,8,9-四氢-4H-焦[1,2-a]嘧啶-4-酮化合物的方法，其盐和水合物

    公开(公告)号：US4456752A

    公开(公告)日：1984-06-26

    申请号：US327689

    申请日：1981-12-04

    申请人： Istvan Hermecz ,  Tibor Breining ,  Lelle Vasvari nee Debreczy ,  Agnes Horvath ,  Jozsef Kokosi

    发明人： Istvan Hermecz ,  Tibor Breining ,  Lelle Vasvari nee Debreczy ,  Agnes Horvath ,  Jozsef Kokosi

    IPC分类号： A61K31/505 ,  A61P11/00 ,  A61P37/08 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： A process for the preparation of nitrogen bridgehead condensed pyrimidine compounds of the general formula ##STR1## [wherein R represents hydrogen or lower alkyl;R.sup.1 represents hydrogen, lower alkyl, carboxy or a derivative thereof or styryl;R.sup.2 represents hydrogen or optionally substituted lower alkyl;R.sup.3 represents hydrogen, optionally substituted lower alkyl, aryl, aralkyl, halogen, carboxy or a derivative thereof, the group --(CH.sub.2).sub.m --COOH (in which m is the integer 1, 2 or 3) or a carboxy derivative thereof, formyl, lower alkanoyl or a condensed thereof;R.sup.4 represents hydrogen, optionally substituted alkyl, aryl optionally substituted by one or more substituents, optionally substituted aralkyl, a heterocyclic group optionally substituted by one or more substituents, the group (CH.sub.2).sub.m --Het (in which m is the integer 1, 2 or 3; Het is an optionally substituted heterocyclic group);R.sup.5 represents hydrogen, C.sub.1-6 alkyl, aryl optionally substituted by one or more substituents, formyl, lower alkanoyl, optionally substituted aroyl or heteroaryl; orR.sup.4 and R.sup.5 together with the nitrogen therebetween represent an optionally substituted mono- or bicyclic heterocyclic ring optionally containing further heteroatom]and pharmaceutically acceptable salts, hydrates, stereoisomers, optically active isomers, geometrical isomers and tautomers thereof.

    摘要翻译： 制备通式为“IMAGE”I的氮桥头浓缩嘧啶化合物的方法[其中R表示氢或低级烷基; R1代表氢，低级烷基，羧基或其衍生物或苯乙烯基; R 2表示氢或任选取代的低级烷基; R 3表示氢，任选取代的低级烷基，芳基，芳烷基，卤素，羧基或其衍生物，基团 - （CH 2）m -COOH（其中m是整数1,2或3）或其羧基衍生物， ，低级烷酰基或其缩合物; R 4表示氢，任选取代的烷基，任选被一个或多个取代基取代的芳基，任选取代的芳烷基，任选被一个或多个取代基取代的杂环基，基团（CH 2）m -Het（其中m是整数1,2 或3; Het是任选取代的杂环基）; R 5表示氢，C 1-6烷基，任选被一个或多个取代基取代的芳基，甲酰基，低级烷酰基，任选取代的芳酰基或杂芳基; 或R4和R5以及它们之间的氮代表任选地被取代的单环或双环杂环，任选地含有另外的杂原子]及其药学上可接受的盐，水合物，立体异构体，光学活性异构体，几何异构体和互变异构体。