Processes for preparing losartan and losartan potassium

Details Processes for preparing losartan and losartan potassium Processes for preparing losartan and losartan potassium

C - Chemistry, Metallurgy

07

D

C07D 403/10 (2006.01) A61K 31/4178 (2006.01) A61P 9/06 (2006.01) A61P 9/10 (2006.01) A61P 9/12 (2006.01)

Patent

CA 2482857

Losartan is prepared by acid catalyzed cleavage of a triarylmethyl group from a triarylmethyl-substituted losartan derivative in a diluent comprising liquid ketone. The reaction mixture is basified and liquid ketone is evaporated from the mixture leaving a residue from which a triarylmethyl alcohol and losartan are each obtained in high yield and high purity. In addition, losartan potassium is prepared by a process that is more convenient that those previously known in the art in which losartan is contacted with potassium ions in substantially pure liquid alcohol and losartan potassium is precipitated from the alcohol.

L'invention porte sur un procédé de préparation de losartan par clivage catalytique acide du groupe triarylméthyle d'un dérivé de losartan à substitution triarylméthyle dans un diluant de cétone liquide. Le mélange réactif est basifié et la cétone liquide du mélange est évaporée, ce qui laisse un résidu dont on tire de l'alcool triarylméthylique et du losartan très pur avec un rendement très élevé. On peu de plus préparer du losartan potassium avec un procédé, plus pratique que ceux pratiqués antérieurement, selon lequel on met en contact le losartan avec des ions potassium dans de l'alcool liquide, le losartan potassium s'obtenant sous forme de précipité.

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