Process for the preparation of racemic citalopram and/or s-...

C - Chemistry – Metallurgy – 07 – D

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C07D 307/87 (2006.01)

Patent

CA 2691149

The invention relates to a process for the preparation of a mixture or R- and S citalopram with more than 50% of the S-enantiomer characterised in that a mixture of R- and S-4--[4-(dimethylamino)-1-(4'-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)-- benzonitrile with more than 50% of the R-enantiomer is subjected to ring closure in presence of an acid. The invention also relates to a process for the preparation of a mixture or R- and S-citalopram with more than 50% of the R-enantiomer characterised in that a mixture of R- and S-4-[4-(dimethylamino)-1-(4'-fluorophenyl)-1- hydroxybutyl]-3--(hydroxymethyl)-benzonitrile with more than 50% of the S-enantiomer is subjected to ring closure in presence of an acid.

La présente invention a pour objet un procédé de préparation d'un mélange de R- et de S-citalopram comportant plus de 50 % de l'énantiomère S, caractérisé par le fait qu'un mélange de R- et de S-4-¬4-(diméthylamino)-1-(4'-fluorophényl)-1-hydroxybutyl|-3-(hydroxyméthyl)-benzonitrile avec plus de 50 % de l'énantiomère R est soumis à une cyclisation en présence d'un acide. La présente invention a aussi pour objet un procédé de préparation d'un mélange de R- et de S-citalopram avec plus de 50 % de l'énantiomère R, caractérisé par le fait qu'un mélange de R- et de S-4-¬4-(diméthylamino)-1-(4'-fluorophényl)-1-hydroxybutyl|-3-(hydroxyméthyl)-benzonitrile avec plus de 50 % de l'énantiomère S est soumis à une cyclisation en présence d'un acide.

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