Process for the preparation of substituted octanoyl amides

Details Process for the preparation of substituted octanoyl amides Process for the preparation of substituted octanoyl amides

C - Chemistry, Metallurgy

07

C

C07C 231/02 (2006.01) C07C 235/34 (2006.01) C07C 247/12 (2006.01) C07C 237/20 (2006.01)

Patent

CA 2412452

Compounds of formula (XII), are simultaneously halogenated in the 5 position and hydroxylated in the 4 position under lactonization, the halolactone is reacted with an amine to form a carboxamide, the halogen is replaced with azide, if necessary after the introduction of a hydroxy protecting group, the resulting azide is converted to a lactone, the lactone is amidated and then the azide converted to the amine group, in order to obtain compounds of formula (I) or a salt thereof.

Selon l'invention, les composés de la formule (XII) sont halogénés simultanément à la position 5 et hydroxylés à la position 4 sous lactonisation ; l'halolactone est mise en réaction avec une amine afin de former un carboxamide ; l'halogène est remplacé par un azide, si nécessaire après introduction d'un groupe de protection hydroxy ; l'azide résultant est transformé en lactone ; et, la lactone est amidée, puis l'azide est transformé en groupe amine afin d'obtenir des composés de formule (I) ou un sel de ces composés.

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