A process for the preparation of zaleplon

Details A process for the preparation of zaleplon A process for the preparation of zaleplon

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01)

Patent

CA 2482545

The invention relates to a process for the preparation of zaleplon (N-[3(3- cyanopyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-N-ethyl-acetamide) in the reaction of 3-dimethylamino-1-(3-N-ethyl-N-acetylaminophenyl)-2-propen-1-one with 3- aminopyrazole-4-carbonitrile, which comprises carrying out said reaction in an aqueous solution of formic acid at formic acid concentrations in the range of 20-80% (w/w). Zaleplon is useful as an anxiolytic, a sedactive and a skeletal muscle relaxant.

L'invention se rapporte à un procédé de préparation de zaleplon (N-[3(3-cyanopyrazolo[1,5-a]pyrimidin-7-yl)phényl]-N-éthyl-acétamide) dans la réaction de 3-diméthylamino-1-(3-N-éthyl-N-acétylaminophényl)-2-propène-1-one avec un 3-aminopyrazole-4-carbonitrile, consistant à réaliser ladite réaction dans une solution aqueuse d'acide formique à des teneurs en acide formique allant de 20 à 80 % masse pour masse. Le zaleplon est utilisé comme anxiolytique, sédatif et calmant des muscles du squelette.

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