Process for the preparation of eburnamonine derivatives

Details Process for the preparation of eburnamonine derivatives Process for the preparation of eburnamonine derivatives

C - Chemistry, Metallurgy

07

D

260/272

C07D 455/00 (2006.01) C07D 461/00 (2006.01) C07D 471/14 (2006.01)

Patent

CA 1252467

A B S T R A C T The invention relates to a new process for the preparation of eburnamonine derivatives of the general Formula I (I) Image (wherein R1 is an alkyl group having 1-6 carbon atoms) and optical and geometrical isomers thereof which comprises reacting a hydroxyimino-octahydro-indolo[2,3-a]quinolizine derivative of the general Formula II Image (II) (wherein R1 is as stated above and R2 stands for an alkyl group having 1-6 carbon atoms being identical with or different from R1, or a hydrogen atom) or an acid addition salt thereof in an organic protic solvent or solvent mixture with an inorganic base, optionally under the addition of water or an aqueous mineral acid, at a temperature between 60 °C and 200 °C. The compounds of the present invention are known drugs having blood pressure decreasing and cerebral vasodilatatory effect. The advantage of the process of the present invention is that it is readily feasible on industrial scale too, provides isomer-free pure products with high yield and requires the use of readily available simple starting materials.

414666

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