Zentiva K.s.

Petr Hruby

Ludek Ridvan

Lukas Placek

Tomas Pekarek

Monika Zatopkova

Stanislav Radl

Lukas Krejcik

Hana Brusova

Natalia Csokova

Anna Zerzanova

Miroslav Kuchar

Lucie Krumbholcova

The invention deals with new salts of the desvenlafaxine base of formula (I) with oxalic acid, the new salts being the hydrogen oxalate of formula (II) in the proportion of desvenlafaxine:oxalic acid of 1:1 and hemioxalate of formula (III) in the proportion of desvenlafaxine:oxalic acid of 2:1. 

Salts of desvenlafaxine and a method of their preparation

A method of preparation of (S)-N-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine of formula (I) or its pharmaceutically acceptable salt, in which (RS)-N,N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine of formula (III) is reacted with an optically active acid, after which a crystallization is made of that diastereoisomer which yields, by reaction with an inorganic or organic base, (S)-N,N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine of formula (S)-III, which is then demethylated using alkylchloroformates, followed by a hydrolysis and optional conversion of the compound of formula (I) to its salt. 

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Prague, Czechia

Petr Hruby