Process for the preparation of alogliptin

Details Process for the preparation of alogliptin Process for the preparation of alogliptin

C - Chemistry, Metallurgy

07

D

C07D 401/04 (2006.01) A61K 31/513 (2006.01) A61P 3/10 (2006.01) C07C 275/24 (2006.01) C07C 275/50 (2006.01) C07D 239/62 (2006.01)

Patent

CA 2755561

The present invention is based on the discovery of a process for preparing pyrimidin- dione compounds, especially alogliptin and its derivatives, which comprises the reaction of a urea derivative of formula (VIII) with a malonic acid or its derivatives to form intermediates of formulae (VII) or (VII-A), which are subsequently converted to a compound of formula (II) upon introduction of a leaving group X. Compound (II) then reacts with an amine to form compound (I), which is optionally converted to its salts of formula (IV).

La présente invention porte sur la découverte d'un procédé permettant de préparer des composés de pyrimidine-dione, en particulier l'alogliptine et ses dérivés, lequel procédé comprend la réaction d'un dérivé de l'urée de formule (VIII) avec un acide malonique ou ses dérivés afin de former des intermédiaires de formules (VII) ou (VII-A), qui sont ensuite convertis en un composé de formule (II) lors de l'introduction d'un groupe partant X. Le composé (II) réagit alors avec une amine de façon à former un composé (I), qui est facultativement converti en ses sels, de formule (IV).

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