Process for introduction of hydroxyethoxy side chain in...

C - Chemistry – Metallurgy – 07 – D

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C07D 239/52 (2006.01) A61K 31/513 (2006.01) A61P 11/00 (2006.01) C07D 403/04 (2006.01)

Patent

CA 2694242

The present invention relates to an improved process for the preparation of bosentan. In particular it relates to a process for preparing bosentan substantially free from the dirner impurity of formula (II) and the 6-hydroxy impurity of formula (III). The invention also relates to a pharmaceutical composition comprising bosentan and its use in the treatment of endothelin-receptor mediated disorders.

La présente invention porte sur un procédé perfectionné pour la préparation de bosentan. En particulier, elle porte sur un procédé pour préparer du bosentan sensiblement exempt de l'impureté dimère de formule (II) et de l'impureté 6-hydroxy de formule (III). L'invention porte également sur une composition pharmaceutique comprenant le bosentan et sur son utilisation dans le traitement de troubles à médiation par les récepteurs de l'endothéline.

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