TH468A - New substance Halovin Camon and the Preparatory Movement - Google Patents

Abstract

This invention pertains to a novel derivative, halovincamone, of general formula (1) ## chemical formula, in which R is an alkyl group of C1-6 (C1-6 alkyl group) and X is a halogen and an acid-forming salt, and is pharmacologically acceptable and optically active isomers. These compounds have a beneficial effect on vasodilation and may have therapeutic applications. The novel compounds described above are prepared according to the method in this invention by a single epimer or epimeric mixture of a racemic or optically active derivative of the halogenate 14-oxo-15-hydroxy-e-homobernane, of general formula (2) ## chemical formula, in which R and X, as described above or the acid-forming salts, are reacted with an oxidizing agent and, if desired, a compound of general formula (1) can be transformed. It can be given as a salt of an increasing and pharmacologically acceptable acid or as an individual isomer.

Claims (3)

1. The process for preparing halogenated-14-oxo-15-hydroxy-E-homoeburnane derivatives with the general formula 1## chemical formula, where R is the alkyl C1-6 group and X is the halogen or the optically active isomer or the pharmaceutically acceptable acid-added salt, is characterized by the single epimer or epimeric mixture of the resinous or optically active derivative of the halogenated-14-oxo-15-hydroxy-E-homoeburnane derivative with the general formula ## chemical formula, where R and X are the above-defined compounds or the aforementioned acid-added salts, is reacted with an oxidizing agent and, if a compound with the general formula (1) is desired, it is converted into a pharmaceutically acceptable acid-added salt or the individual isomers are separated. 2. The process described in claim 1 is characterized by the use of reactive manganese dioxide as an oxidizing agent. 3. The process of preparing pharmaceutical components with vasodilating effects is characterized by the general formulation (1) where R is a C1-6 alkyl group and X is a halogen or derivative that is clearly optically active or a pharmaceutically acceptable acid-added salt being transformed into a pharmaceutical component by commonly known methods using common pharmaceutical carriers and/or diluents (3 claims, drawing - picture).