Hexahydroindoloquinolizinium and octahydroindoloquinolizine este

Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Bacterium or component thereof or substance produced by said...

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546 51, 546 70, A61K 31435, C07D45500

Patent

active

044461399

ABSTRACT:
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.

REFERENCES:
patent: 3755333 (1973-08-01), Szantay et al.
patent: 4035370 (1977-07-01), Lorincz et al.
patent: 4173642 (1979-11-01), Szantay et al.
patent: 4190658 (1980-02-01), Warnant et al.
patent: 4345082 (1982-08-01), Szantay et al.

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