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    Method of preparing n-oxo-tetrahydro-beta-carbolines
    5.
    发明授权
    Method of preparing n-oxo-tetrahydro-beta-carbolines 失效
    制备N-氧代四氢 - 碳 - 碳的方法

    公开(公告)号：US5106840A

    公开(公告)日：1992-04-21

    申请号：US533415

    申请日：1990-06-05

    申请人： Peter H. H. Hermkens ,  Jan H. Van Maarseveen ,  Johan W. Scheeren ,  Cornelis G. Kruse

    发明人： Peter H. H. Hermkens ,  Jan H. Van Maarseveen ,  Johan W. Scheeren ,  Cornelis G. Kruse

    IPC分类号： C07D209/14 ,  A61K31/435 ,  A61K31/535 ,  A61K31/55 ,  A61P31/12 ,  A61P35/00 ,  C07D498/14 ,  C07D499/14 ,  C07D515/14

    CPC分类号： C07D515/14

    摘要： The invention relates to a method of preparing N-oxo-tetrahydro-.beta.-carbolines having formula 1. ##STR1## wherein R.sub.1 is lower alkyl or alkoxy, halogen, trifluoromethyl, lower alkylthio, hydroxy, amino, lower mono- or dialkyl- or acylamino.n has the value 0, 1 or 2,R.sub.2 is hydrogen, lower alkyl or acyl,R.sub.3 is hydrogen, lower alkyl or alkoxycarbonyl, or a phenyl group optionally substituted with a group R.sub.1, andA together with the group --C--N--O--, forms a saturated heterocyclic ring systems consisting of 6-8 ring atoms, wherein, in addition to the already present oxygen atom and nitrogen atom, an extra hetero atom from the group, O, S and N may be present, which ring system may be substituted with one or more of the substituents alkyl, alkoxycarbonyl, alkanoyl, alkoxy, hydroxy, oxo, amino, mono- or dialkylamino, alkanoyl-or alkoxycarbonylamino, which ring system may be annelated with a saturated carbocyclic group of 5 or 6 ring atoms, by an intramolecular ring closure reaction of compounds of formula 2 ##STR2## wherein Z is an aldehyde function or acetal function, or is a functional group which can be converted into such a funciton during the ring closure reaction.The eudistomin derivatives within the group of compounds having formula 1 have strong antiviral and antitumor activity.