Process for the preparation of hydroxyamino-eburnane derivatives

Details Process for the preparation of hydroxyamino-eburnane derivatives Process for the preparation of hydroxyamino-eburnane derivatives

1980-05-29

1982-08-17

Daus, Donald G.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

546 70, 424256, C07D46100, C07D45500, A61K 31475

Patent

active

043450822

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.

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