Intermediate compound for synthesizing pharmaceutical agent...

C - Chemistry – Metallurgy – 07 – D

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C07D 265/30 (2006.01) C07D 265/32 (2006.01)

Patent

CA 2615515

The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps: wherein each symbol is as defined in the specification. The present invention also relates to a production method of an compound represented by the formula 55, which includes the following steps: wherein each symbol is as defined in the specification. According to the production method of the present invention, an optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1- methyl-1H-[4,4']bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.

La présente invention concerne un procédé de production d'un composé morpholine optiquement actif représenté par la formule (10) qui comprend les étapes suivantes dans lesquelles chaque symbole est tel que défini dans le descriptif. Cette invention porte également sur un procédé de production d'un composé représenté par la formule (55) qui comprend les étapes suivantes dans lesquelles chaque symbole est tel que spécifié dans le descriptif. Conformément au procédé de production selon l'invention, un composé morpholine à substitution 2 aryle optiquement actif et un 3-oxo-3-(pyrimidin-4-yl)propionate qui sont importants en tant que produits de départ pour la synthèse de 2-(2-arylmorpholin-4-yl)-1-méthyl-1H-[4,4']bipyrimidinyl-6-one présentant une activité inhibitrice de la tau protéine kinase 1 et utile en tant que médicament thérapeutique pour la maladie d'Alzheimer et similaire peuvent être produits à haut rendement par un procédé avantageux du point de vue industriel. Formule (10)

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