Process for the manufacture of sertraline

Details Process for the manufacture of sertraline Process for the manufacture of sertraline

C - Chemistry, Metallurgy

07

C

C07C 209/24 (2006.01)

Patent

CA 2485499

Process for the preparation of sertraline by reductive amination of racemic 4- (3, 4-dichlorophenyl)-3, 4-dihydro-1-(2H)-naphthalenone, carried out as one- reaction-vessel process without isolation of intermediates, in the form of pure separated cis and trans isomers, the way of conversion of trans isomer to cis isomer and preparation of FII polymorph of 1S-cis isomer from any other polymorph.

L'invention concerne un procédé de préparation de sertraline par amination réductrice de 4-(3, 4-dichlorophényl)-3, 4-dihydro-1-(2H)-naphtalènone racémique, réalisée de façon monotope sans isolation des intermédiaires, sous forme d'isomères purs cis et trans séparés. Elle concerne aussi la voie de conversion de l'isomère trans en isomère cis et la préparation du polymorphe FII de l'isomère 1S-cis à partir d'un autre polymorphe quelconque.

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