| 摘要 |
PURPOSE: An improved method for the manufacture of metoprolol base that uses no other solvents than water for the reaction of p-(2-methoxyethyl)phenol and epichlorohydrin is provided. The method is environmentally sound and gives a good yield and high purity. CONSTITUTION: A method for the manufacture of metoprolol comprises : (i) reacting in a first step p-(2-methoxyethyl)phenol and epichlorohydrin in water as solvent and at a temperature of 50 to 700°C, evaporating the excess of epichlorohydrin and then distilling the obtained 1 -(2,3 -epoxypropoxy)-4-(2-methoxyethyl)-benzene under reduced pressure, and (ii) in a second step reacting the obtained l-(2,3-epoxypropoxy)-4 (2-methoxyethyl)-benzene and isopropylamine is the presence of isopropyl alcohol to form metoprolol base.
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