C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 487/04 (2006.01) C07C 231/08 (2006.01) C07C 233/43 (2006.01) C07D 231/00 (2006.01) C07D 239/00 (2006.01)
Patent
CA 2381524
Methods of making substituted pyrazolopyrimidines generally and, more particularly, N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-.alpha.]- pyrimidin-7-yl}phenyl)acetamide. Such compounds have utility over a wide range of indications, including treatment of insomnia. In the practice of the present invention, improved techniques which do not require use and/or isolation of the pyrazole intermediate are disclosed, as well as improved techniques for making the reaction intermediates themselves. Such techniques offer significant advantages, including enhanced efficiency, particularly in the context of large scale manufacture.
La présente invention concerne des procédés de fabrication de pyrazolopyrimidines substituées, et plus particulièrement de N-méthyl-N-(3-{3-[2-thiénylcarbonyl]-pyrazol-[1,5-.alpha.]-pyrimidin-7-yl}phényl)acétamide. Ces composés conviennent pour une famille d'indications, et notamment le traitement de l'insomnie. L'invention concerne également, sous son aspect pratique, d'une part des procédés améliorés évitant l'utilisation et/ou l'isolation de l'intermédiaire pyrazole, et d'autre part des perfectionnements techniques de fabrication des intermédiaires de réaction. Ces améliorations techniques présentent l'avantage d'une meilleure efficacité, notamment dans le cadre d'une production à grande échelle.
Gross Raymond S.
Oglesby Richard Christopher
Wilcoxen Keith M.
Gowling Lafleur Henderson Llp
Neurocrine Biosciences Inc.
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