C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 243/14 (2006.01) C07D 487/04 (2006.01)
Patent
CA 2373506
The present invention relates to a process for manufacturing diazepine derivatives of general formula (I) wherein R1 is lower alkyl and R2 is hydrogen, or R1 and R2 are together -(CH2)n, and n is 2 or 3; R3 is halogen, lower alkyl, lower alkoxy and m is 0, 1 or 2; R4 is hydrogen or lower alkyl. The compounds of general formula (I) are valuable intermediate products for the manufacture of imidazo[1,5-a][1,4]diazepine derivatives, like for instance 7-chloro-3-(5-dimethylaminomethyl-[1, 2,4]oxadiazol-3-yl)-5-methyl-4,5-di- hydro -imidazo[1,5-a][1,4]benzodiazepin-6-one, which diazepine derivatives show excellent psychopharmacological properties as agonists of the central benzodiazepine receptors.
La présente invention concerne un procédé de fabrication de dérivés de la diazépine de formule générale (I) dans laquelle R<1> est alkyle inférieur et R<2> est hydrogène, ou R<1> et R<2> sont ensemble -(CH2)n- et n est 2 ou 3; R<3> est halogène, alkyle inférieur, alkoxy inférieur et m est 0, 1 ou 2; R<4> est hydrogène ou alkyle inférieur. Ces composés de formule générale (I) constituent des produits intermédiaires précieux pour la fabrication de dérivés de la imidazo[1,5-a][1,4]diazépine, tels que le 7-chloro-3-(5-diméthylaminométhyl-[1,2,4]oxadiazol-3-yl)-5-méthyl-4,5-dihydro-imidazo[1,5-a][1,4]benzodiazépine-6-one. Ce dérivé de la diazépine présente de remarquables propriétés psychopharmaceutiques en tant qu'agonistes des récepteurs centraux des benzodiazépines.
Borden Ladner Gervais Llp
F. Hoffmann-La Roche Ag
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