Halovincamone derivatives and a process for the preparation...

C - Chemistry – Metallurgy – 07 – D

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C07D 461/00 (2006.01)

Patent

CA 1152076

ABSTRACT OF THE DISCLOSURE The invention relates to new halovincamone derivat- ives of the general formula (I), Image (I) wherein R is a C1-6 alkyl group and X is halogen, and phar- maceutically acceptable acid addition salts and optically active isomers thereof. These compounds possess valuable vasodilating effect, and can be applied to advantage in the therapy. The new compounds defined above are prepared accord- ing to the invention so that a single epimer or an epimeric mixture of a racemic or optically active halogenated 14-oxo- 15-hydroxy-E-homoeburnane derivative of the general formula (II), Image (II) wherein R and X are as defined above, or an acid addition salt thereof is treated with an oxidizing agent, and, if desired, the resulting compound of the general formula (I) is converted into its pharmaceutically acceptable acid addi- tion salt and/or resolved.

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