Synthesis methods and intermediates for the manufacture of...

Details Synthesis methods and intermediates for the manufacture of... Synthesis methods and intermediates for the manufacture of...

C - Chemistry, Metallurgy

07

D

C07D 209/16 (2006.01) C07D 403/06 (2006.01)

Patent

CA 2553652

The invention relates to a process for the manufacture of an 1,2,4-triazol-1- yl compound of the formula [A], or a salt thereof, wherein each of R3 and R4 is hydrogen or lower alkyl, said process comprising reacting a hydrazine compound of the formula [B] wherein R is hydrogen or acyl, R2 is hydrogen or a protecting group, are hydrogen or lower alkyl, and R6 is hydrogen or COOR7, or a salt thereof, with a 1,2,4-triazolyl forming reagent. In addition, novel intermediates for the synthesis of the anti-migraine agent Rizatriptan and methods for their synthesis are presented.

L'invention concerne un procédé pour préparer un composé 1,2,4-triazol-1-yl de formule [A] ou un sel de ce composé de formule [A], chaque R3 et R4 dans ladite formule [A] désignant hydrogène ou un alkyle inférieur. Le procédé selon l'invention comprend l'étape qui consiste à faire réagir un composé hydrazine de formule [B] dans laquelle R représente hydrogène ou acyl, R2 désigne hydrogène ou un groupe de protection, R3 et R4 représentent hydrogène ou un alkyle inférieur, et R6 désigne hydrogène ou COOR7, ou un sel de ce composé de formule [B], avec un réactif formant le composé 1,2,4-triazolyl. La présente invention se rapporte en outre à de nouveaux produits intermédiaires pour synthétiser l'agent antimigraineux Rizatriptan, ainsi qu'à des procédés de synthèse correspondants.

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