| 摘要 |
<p>The invention relates to highly pure, crystalline, stable compounds of 3,3-diphenylpropylamine derivatives, in the form of their salts of general formula (I), a method for production of highly pure, stable, intermediate products of general formula (1). The compound of general formula (III) is decomposed by hydrogenation agent in order to produce the compound of general formula (VI) that is changed by acylation agent into the compound of the general formula (A) and that is changed with help of physiologically compatible inorganic or organic acid into the compound of general formula (I). The method is particularly characterized by regio- and chemo-selectivity and high yields and provides salts of phenolic monoesters of 3,3-diphenylpropylamines, which are particularly suitable for application in technical pharmaceutic formulations. Preferred compounds are R-(+)-2-(3-diisopropylamino-1-phenylpropyl)-4- hydroxymethylphenyl isobutyrate hydrogenfumarate and R-(+)-2-(3- diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenyl isobutyrate hydrochloride hydrate. The method further provides essential, stable, crystalline intermediate products for the production of the above salts.; A preferred intermediate product is R-(-)-3-(3-diisopropylaminophenylpropyl)-4-hydroxybenzoic acid methyl ester.</p> |
