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    • 1. 发明授权
    • Nitrogen-containing polycyclic compounds and a process for the
preparation thereof
    • 含氮多环化合物及其制备方法
    • US4054571A
    • 1977-10-18
    • US614151
    • 1975-09-17
    • Csaba SzantayLajor SzaboGyorgy KalausEgon KarpatiLaszlo Szporny
    • Csaba SzantayLajor SzaboGyorgy KalausEgon KarpatiLaszlo Szporny
    • C07D471/06A61K31/4375A61K31/4745C07D461/00C07D471/04
    • C07D461/00
    • The invention relates to new eburnamenine derivatives of the general formula (I), ##STR1## wherein R.sub.1 stands for an alkyl group,R.sub.2 stands for a carboxy group, a functional carboxy derivative (preferably an ester group) or a group convertable into carboxy group or a functional derivative thereof (preferably cyano group), andX.sup.- is an anion derived from an acid,And the corresponding free bases.These compounds are valuable intermediates of the preparation of eburnamenine derivatives with advantageous therapeutical effects.The above compounds are prepared as follows: a compound of the general formula (II), ##STR2## wherein R.sub.1 has the same meanings as defined above, is reacted with a compound of the general formula (III), ##STR3## wherein R.sub.2 has the same meanings as defined above and Y is halogen, and, if desired, a thus-obtained compound of the general formula (I), wherein R.sub.1 and R.sub.2 each have the same meanings as defined above and X.sup.- is a halide ion, is reacted with an acid, and/or, if desired, a compound of the general formula (I), wherein R.sub.1 and X.sup.- each have the same meanings as defined above and R.sub.2 is cyano or an ester group, is subjected to hydrolysis, and/or, if desired, a compound of the general formula (I), wherein R.sub.1, R.sub.2 and X.sup.- each have the same meanings as defined above, is treated with a base.
    • 本发明涉及通式(I),其中R1代表烷基,R2代表羧基,官能羧基衍生物(优选酯基)或可转化基团的新颖的本本母胺衍生物 羧基或其功能性衍生物(优选氰基),X是衍生自酸的阴离子,和相应的无碱基。