Process for the preparation of 11-bromo-vincaminic acid ester de

Details Process for the preparation of 11-bromo-vincaminic acid ester de Process for the preparation of 11-bromo-vincaminic acid ester de

1979-07-11

1981-08-11

Jiles, Henry R.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Bacterium or component thereof or substance produced by said...

2602393P, 546 51, 546 70, A61K 3155, C07D45900, C07D46100

Patent

active

042834015

ABSTRACT:
A novel process for preparing 11-bromo-vincaminic acid esters of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each stand independently from each other for a C.sub.1-6 alkyl group, comprising the steps of treating a 1-alkyl-1-alkoxycarbonylethyl-octahydroindolo-quinolisine of the general formula ##STR2## wherein R.sup.2 is as defined above and R.sup.3 stands for a C.sub.1-6 alkyl group, with a brominating agent and treating the resulting isomeric mixture of the bromo-derivatives with an alkaline agent or treating the corresponding 14-oxo-E-homo-eburnane being unsubstituted in ring A with a brominating agent and nitrosating the resulting 11-bromo-14-oxo-E-homo-eburnane of the general formula ##STR3## wherein R.sup.2 is as defined above, then subjecting the resulting 11-bromo-14-oxo-15-hydroxyimino-E-homoeburnanes to deoxyimination and treating the 14,15-dioxo-derivatives obtained with a base in an alcohol of the general formula R.sup.1 OH, wherein R.sup.1 is as defined above.
All the intermediate products are novel and exhibit a therapeutical protecting effect against cerebral hypoxy.

REFERENCES:
patent: 3770724 (1973-11-01), Warnant et al.
patent: 4146643 (1979-03-01), Pfaffli

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