Process for preparing 10-halogen-e-homo eburnanes

Details Process for preparing 10-halogen-e-homo eburnanes Process for preparing 10-halogen-e-homo eburnanes

C - Chemistry, Metallurgy

07

D

260/241.1

C07D 459/00 (2006.01) C07D 471/22 (2006.01)

Patent

CA 1140121

ABSTRACT OF THE DISCLOSURE The invention relates to new 10-halo-E-homoeburnane derivatives of the general formula (I), Image (I) wherein R2 is a C1-6 alkyl group and X is halogen, and epimers, optically active derivatives and pharmaceutically acceptable acid addition salts thereof. These substances exert vasodilating effects and can be applied to advantage in the therapy. The new compounds are prepared so that a racemic or optically active 9-halo-octahydroindoloquinolisine derivative of the general formula (II), Image (II) wherein R2 and X are as defined above and R1 is a C1-6 alkyl group, or an acid addition salt thereof is treated with a strong base, and, if desired, the 15- epimers of the resulting compound having the general formula (I) are separated from each other, and/or, if desired, the resulting substance is converted into its pharmaceutically acceptable acid addition salt and/or resolved.

358098

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