NOVEL METHOD FOR METOPROLOL PRODUCTION Russian patent published in 2003 - IPC

FIELD: organic chemistry, chemical technology, medicine, pharmacy. SUBSTANCE: invention relates to the improved method for preparing metoprolol that is the known medicinal agent used in treatment of patients with arrythmia and myocardium infarct. At the first stage p-(2-methoxyethyl)-phenol and epichlorohydrin are subjected for interaction in water as a solvent in the coarse of a base addition and excess of epichlorohydrin is evaporated at temperature 50-70 C and obtained 1-(2,3-epoxypropoxy)-4-(2-methoxyethyl)benzene is distilled then under reduced pressure. At the first stage prepared 1-(2,3-epoxypropoxy)-4-(2- methoxyethyl)benzene is subjected for interaction with isopropylamine to yield metoprolol-base that if necessary is converted to metoprolol tartrate or metoprolol succinate. Usually, the first stage is carried out in the presence of sodium hydroxide or potassium hydroxide. Prepared metoprolol-base can be purified by dissolving metoprolol-base in solvent taken among toluene, isobutylmethyl ketone and butyl acetate and extraction with solution of hydrochloric or sulfuric acid. Method is safe ecologically and allows preparing the end product with good yield and high purity degree. EFFECT: improved preparing method. 6 cl