Gepefrine

Originator

Pressionorm,Helopharm,W. Germany,1981

Manufacturing Process

Hydrolysis of D-(+)-1-(3-rnethoxyphenyl)-2-aminopropane: 2.42 mols (40 g) of the compound are dissolved in 6N hydrochloric acid in a bomb tube consisting of stainless steel and having a capacity of 500 ml. Hydrogen chloride gas is passed into the ice-cooled solution until this is saturated, The solution is then heated to 130°C for 2 hours in an air bath. After cooling and driving off the hydrochloric acid at a slightly elevated temperature, the hydrochloride of the 3-hydroxyphenyl derivative is present in the form of a yellowish syrup.
The free base can be liberated from the hydrochloride by extracting a butanol solution of the hydrochloride several times with sodium bicarbonate solution. After recrystallization from isopropanol/ligroin, the yield of D-(+)-1-(3- hydroxyphenyl)-2-aminopropane amounts to 33.0 g, corresponding to 90.1% of theory relative to the D-form. Melting point = 152°C to 154°C.

Therapeutic Function

Antihypotensive