C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/272
C07D 471/16 (2006.01) C07D 461/00 (2006.01) C07D 471/14 (2006.01)
Patent
CA 1148157
ABSTRACT OF THE DISCLOSURE The invention relates to new hydroxyamino-eburnene derivatives of the general formula (I), Image (I) wherein R1 and R2 each stand for a C1-6 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-indolo- quinolisinium derivative of the general formula (II), Image (II) wherein R2 is as defined above and X stands for an acid residue, with a methylenemalonic acid diester derivative of the general formula (III), - 2 - Image (III) wherein R1 is as defined above, subjecting the resulting product to catalytic hydrogenation, treating the resulting product with an alkali, and reacting the resulting octa- hydroindoloquinolisine monoester derivative with a nitrosat- ing agent in an acidic medium.
353141
Dancsi Lajos
Gazdag Maria
Kalaus Gyorgy
Keve Tibor
Sapi Janos
Fetherstonhaugh & Co.
Richter Gedeon Vegyeszeti Gyar Rt
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