GB789427A - Process for the preparation of a biologically active compound - Google Patents

Abstract

A biologically active hypotensive substance which is a colourless glittering crystalline solid having an acicular and prism-like structure, a melting-point between 153 DEG and 155 DEG C., [a ]21D in acetone of +367 DEG , [a ]21D in chloroform of +369 DEG , and an absorption spectrum in absolute ethyl alcohol with maxima at 225 and 317 mm , is extracted from plants of the oleaceae family, e.g. olea europa, olives. Selected parts of the plants, e.g. bark, leaves, roots or fruits, or an extract of these parts in water or a water-miscible organic solvent, e.g. ethanol, acetone, are extracted with a non-water-miscible organic solvent, e.g. chloroform, methylene chloride, carbon tetrachloride and benzene, evaporating the separated non-water-miscible organic solvent, distilling the oily residue, if desired after a further purification, in vacuo and separating the fraction distilling between 120 DEG and 160 DEG C. at 0.1 mm. mercury and bringing this fraction to crystallization. The extract of the plants in water or a water-miscible organic solvent may be subjected to an acid hydrolysis using an organic aliphatic acid, e.g. acetic, butyric, succinic or citric acid, or an inorganic acid, e.g. phosphoric, hydrochloric or sulphuric acid, or a cation exchanger in the acid form, e.g. Dowex-50. The extract in the non-water-miscible organic solvent may be purified by evaporation, extracting the oily residue with water, extracting the filtered separated aqueous solution with ether and evaporating the ethereal extract and distilling the oily residue in vacuo as before. The hypotensive substance may be administered orally or parenterally as tablets, solutions, suspensions or isotonic aqueous solutions, in admixture with normal excipients, e.g. gelatin, starch, lactose, cane sugar, talcum powder, stearic acid, magnesium stearate and physiological salt solutions.