An improved process for preparation of irbesartan

Details An improved process for preparation of irbesartan An improved process for preparation of irbesartan

C - Chemistry, Metallurgy

07

D

C07D 403/10 (2006.01) A61K 31/4184 (2006.01) A61P 9/00 (2006.01) C07C 13/10 (2006.01)

Patent

CA 2604404

A process for the preparation of Irbesartan of formula (I): Formula (I) comprising the steps of: (i) reacting 4' aminomethyl-2-cyano biphenyl of formula (VI) with 1-veleramido cyclopentane carboxylic acid of formula (V): Formula (VI) & Formula (V) in an organic solvent and in the presence of an acid, without activating the -COOH group of compound of formula (V) to give 1- (2'cyanobiphenyl-4-yl-methylaminocarbonyl)-1-pentanoylamino cyclopentane of formula (VII). Formula (VII) converting the compound of formula (VII) obtained in step (i) to Irbesartan of formula (I) by reacting the compound of the formula (VII) with tributyl tin azide in o-xylene to give Irbesartan of formula (I).

L~invention concerne un procédé pour la préparation d'Irbésartan de formule (I) [Formule (I)], comprenant les étapes consistant à : (i) faire réagir du 4'-aminométhyl-2-cyanobiphényle de formule (VI) avec de l'acide 1-valéramidocyclopentanecarboxylique de formule (V) [Formule (VI) & Formule (V)] dans un solvant organique et en présence d'un acide, sans activer le groupe -COOH du composé de formule (V) pour produire du 1-(2'-cyanobiphényl-4-yl-méthylaminocarbonyl)-1-pentanoylaminocyclopentane de formule (VII) [Formule (VII)] ; (ii) convertir le composé de formule (VII) obtenu dans l'étape (i) en Irbésartan de formule (I) en faisant réagir le composé de formule (VII) avec de l'azoture de tributylétain dans de l'o-xylène pour produire de l'Irbésartan de formule (I).

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