Process for the preparation of vincaminic acid esters

Details Process for the preparation of vincaminic acid esters Process for the preparation of vincaminic acid esters

1982-09-28

1984-08-07

Daus, Donald G.

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

546 70, C07D46100, C07D45500

Patent

active

044645341

ABSTRACT:
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) ##STR1## in which R.sup.1 and R.sup.2 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) ##STR2## in which R.sup.1 and R.sup.2 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.degree. to 110.degree. 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.

REFERENCES:
patent: 3755333 (1973-08-01), Szantay et al.
patent: 3770724 (1973-11-01), Warnant et al.
patent: 4146643 (1979-03-01), Pfaffli
patent: 4283401 (1981-08-01), Szantay et al.
patent: 4314939 (1982-02-01), Szantay et al.
patent: 4316029 (1982-02-01), Rossey

Affiliated with

Also associated with

Rating

Process for the preparation of vincaminic acid esters does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Process for the preparation of vincaminic acid esters, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Process for the preparation of vincaminic acid esters will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-604510