Method for synthesis of omeprazole

Details Method for synthesis of omeprazole Method for synthesis of omeprazole

C - Chemistry, Metallurgy

07

D

C07D 401/12 (2006.01)

Patent

CA 2083605

The present invention relates to an improved method for the synthesis of omeprazole, comprising the steps of reacting 5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridinyl)- methylthlo]-1H-benzimidazole with m-chloroperoxy-benzoic acid in a methylene chloride solution at a substantially constant pH of about 8.0 to 8.6; extracting the reaction mixture with aqueous NaOH; separating the aqueous phase from the organic phase; and adding an alkyl formate to the aqueous phase, resulting in crystallization of omeprazole. (see fig. I)

La présente invention porte sur une méthode améliorée pour la synthèse de l'oméprazole, consistant à faire réagir le 5-méthoxy-2-¢(4-méthoxy-3,5-diméthyl-2-pyridinyl)méthylthio!-1H-benzimidazole avec l'acide m-chloroperoxybenzoïque dans une solution de chlorure de méthylène, à un pH pratiquement constant d'environ 8,0 à 8,6; à soumettre le mélange réactionnel à une extraction avec NaOH aqueux; à séparer la phase aqueuse de la phase organique; enfin, à ajouter un formiate d'alkyle à la phase aqueuse, entraînant la cristallisation de l'oméprazole (voir fig. I).

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