Novel processes and intermediates for the preparation of...

C - Chemistry – Metallurgy – 07 – D

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C07D 419/04 (2006.01) C07D 241/04 (2006.01) C07D 401/12 (2006.01)

Patent

CA 2191874

Compounds having the formula R5O-A-NR4-R2 (V), where R2 is a heteroaryl group linked to the remainder of the molecule via a carbon atom adjacent a nitrogen atom and R4 and R5 are both hydrogen atoms or together represent -SO- or -SO2- and A is C2-C4 alkylene optionally substituted by one or more lower alkyl groups are novel intermediates in the preparation of pharmaceutically useful piperazine derivatives as end compounds. The compounds having formula (V) where R4 and R5 are hydrogen may be prepared by a rearrangement of a compound having the formula R2-O-A-NH2 (VI).

On décrit des composés de formule R<5>O-A-NR<4>-R<2> (V) où R<2> représente un groupe hétéroaryle lié au reste de la molécule par l'intermédiaire d'un atome de carbone adjacent à un atome d'azote, et R<4> et R<5> représentent chacun des atomes d'hydrogène ou ensemble -SO- ou -SO2-, et A représente alkylène C2-4 éventuellement substitué par un ou plusieurs groupes alkyle inférieur. Ces composés constituent de nouveaux intermédiaires dans la préparation de composés finals, des dérivés de pipérazine pharmacologiquement utiles. Les composés de formule (V), où R<4> et R<5> représentent hydrogène, peuvent être préparés par un réarrangement d'un composé de formule (VI): R<2>O-A-NH2.

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