process for the manufacture of an indole alkaloid and its salt and its application as medicine

摘要

1350869 Salts based on descarbomethoxy dihydrovabasine AGENCE NATIONALE DE VALORISATION DE LA RECHERCHE 13 March 1972 [12 March 1971] 11600/72 Heading C2C Novel salts of a compound I with a mineral or organic acid are prepared by extraction of the total alkaloids of dried root barks of Hazunta silicicola Pich with ether, methylene chloride or CHCl 3 , chromatography of the mixture on alumina, elution and conventional treatment of the appropriate fractions to give the required salts. Alternatively the dried root barks may be made alkaline and extracted with ether methylene chloride or CHCl 3 ; the extract is then concentrated and extracted with 10% aqueous sulphamic acid or 2-5% aqueous sulphuric acid; the acid solution is washed with ether, made alkaline with NH 3 and the precipitated alkaloids extracted with ether, methylene chloride or CHCl 3 ; the extract is chromatographed on alumina and eluted with benzene; and the resulting mixture of descarbomethoxyvobasine and descarbomethoxydihydrovobasine (I) is recrystallized from methanol, followed by salt formation. The hydrochloride of I may be prepared by dissolution of the dried root barks in methanol; addition of HCl until a pH of about 1 is obtained, and recrystallization of the crystals formed from methanol. Pharmaceutical compositions comprise a salt of I together with a suitable carrier or diluent and are administered in the form of tablets, pills, capsules, solutes, emulsions, syrups or suppositories. They are useful in treating hypertension, progressive cerebral insufficiency, vertigo, earbuzzing, disorders of memory, chronic cerebrosclerosis and disorders of consciousness of cranium traumatisms.