C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 487/00 (2006.01)
Patent
CA 2553465
An improved method of making a substituted pyrazolopyrimidine. The method comprises reacting a aminopyrazole compound or a salt thereof with a substituted 1-oxo-2-propenyl-arene(-heterocycle) or a salt thereof under acidic conditions in a reaction medium including a two-phase mixture of an aqueous solution and a water-immiscible organic liquid. Specific substituted pyrazolopyrimidines include N-[3-(3-cyanopyrazolo[1,5-a]pyrimidin-7-yl)phenyl]- N-ethylacetamide and N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazolo[1, 5-a]- pyrimidin-7-yl}phenyl)acetamide.
L'invention concerne un procédé amélioré de fabrication de pyrazolopyrimidine substituée. Le procédé consiste à faire réagir un composé d'aminopyrazole ou un sel de celui-ci avec un 1-oxo-2-propényl-arène(-hétérocycle) ou un sel de celui-ci dans des conditions acides, dans un milieu de réaction comprenant un mélange à deux phases d'une solution aqueuse et d'un liquide organique miscible à l'eau. Des pyrazolopyrimidines spécifiques substitués comprennent N-[3-(3-cyanopyrazolo[1,5-a]pyrimidin-7-yl)phényl]-N-éthylacétamide et N-méthyl-N-(3-{3-[2-thienylcarbonyl]-pyrazolo[1, 5-a]-pyrimidin-7-yl}phényl)acétamide.
Cantrell Gary Lee
Halvachs Robert Edward
Moser Frank William
Mallinckrodt Inc.
Osler Hoskin & Harcourt Llp
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