A PROCESS FOR THE PREPARATION OF DULOXETIN AND NEW KEY INTERMEDIATES FOR USE THEREIN

A PROCESS FOR THE PREPARATION OF DULOXETIN AND NEW KEY INTERMEDIATES FOR USE THEREIN

The present invention relates to a process for the preparation of duloxetin. ((S)-(+)-N-methyl-N-(3-(l-na?hthalenyloxy)-3-(2-thienyl)propanamine) of formula (I) and pharmaceutically acceptable salts thereof, said process comprising the steps of a) resolving racemic 3-(N-methyl-N-berizylamino)-1-(2-t...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: SCHINDLER, JOZSEF, FARAGO, JANOS, TEMESVARI, KRISZTINA, GATI, TAMAS, VUKICS, KRISZTINA, BODI, JOZSEF, ELES, JANOS, SZOEKE, KATALIN, FOGASSY, ELEMER
Format: Patent
Sprache:eng ; fre ; ger
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:The present invention relates to a process for the preparation of duloxetin. ((S)-(+)-N-methyl-N-(3-(l-na?hthalenyloxy)-3-(2-thienyl)propanamine) of formula (I) and pharmaceutically acceptable salts thereof, said process comprising the steps of a) resolving racemic 3-(N-methyl-N-berizylamino)-1-(2-thienyl)-1-propanol of formula (II) with a D-phenylglycine derivative to obtain a compound of formula (IV); and b) reacting (S)-3-(N-methyl-N-ben2yIamino)-1-(2-thienyl)-1-propanol of formula (IV) with 1-fluoronaphthalene to yield (S)-N-methyl-N-benzyl-3-(1-naphthalenyloxy)-3-(2- thienyl)propanamine of formula (V), reacting the compound of formula (V) obtained with 1-chloroethyl chloroformate to yield duloxetin of formula (I), and if desired converting the duloxetin of formula (I) obtained into an acid addition salt thereof.