FREMGANGSMAADE TIL FREMSTILLING AF VINCAMINSYREESTERE

The invention relates to a new process for the preparation of apovincaminic acid esters. More particularly, the invention concerns a process for preparing racemic and optionally active vincaminic acid esters of the formula (I) (I) in which R1 and R2 independently stand for alkyl having from one to 6...

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Main Authors SZABO LAJOS, FARKAS MARIA, VISKY GYOERGY, SZANTAY CSABA, KREIDL JANOS, KALAUS GYOERGY, CZIBULA LASZLO, NEMES ANDRAS
Format Patent
LanguageDanish
Published 31.03.1983
Edition3
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:The invention relates to a new process for the preparation of apovincaminic acid esters. More particularly, the invention concerns a process for preparing racemic and optionally active vincaminic acid esters of the formula (I) (I) in which R1 and R2 independently stand for alkyl having from one to 6 carbon atoms, and 14-epimers thereof. According to the invention an octahydroindolo[2,3-a]quinolizine-oxime ester of the formula (II) (II) in which R1 and R2 have the same meaning as defined above, is reacted with an aqueous solution of sulfurous acid or a salt thereof at a temperature of 80 DEG to 110 DEG C. and the 14-epimeric mixture obtained is epimerized or separated in a known manner and if desired, the racemic vincaminic acid esters are resolved. The valuable, pharmaceutically active compounds of the formula (I) can be prepared according to the invention in a considerably improved yield and the undesired side reactions can be suppressed and/or the by-products can easily be converted into other pharmaceutically active materials.
Bibliography:Application Number: DK19820004316