Process for the production of zaleplon

C - Chemistry – Metallurgy – 07 – D

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C07D 487/08 (2006.01) C07D 487/04 (2006.01)

Patent

CA 2450384

The present invention provides a process for the production of N-[3(3- cyanopyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-N-ethylacetamide (zaleplon), an active ingredient that is approved for the treatment of insomnia. The process involves reacting N-[3-[3-(dimethylamino)-1-oxo-2-propenyl]phenyl]-N- ethylacetamide or a salt thereof with 3-amino-4-cyanopyrazole or a salt thereof under acidic conditions in a reaction medium comprising a mixture of water and a water-miscible organic compound.

La présente invention concerne un procédé de production de N-[3(3-cyanopyrazolo[1,5-a]pyrimidine-7-yle)phényle]-N-éthylacétamide (Zaleplon), en l'occurrence, un principe actif approuvé pour le traitement de l'insomnie. En l'occurrence, on prend du N-[3-[3-(diméthylamino)-1-oxo-2-propényle]phényle]-N-éthylacétamide, ou l'un de ses sels, et on le fait réagir avec du 3-amino-4-cyanopyrazole, ou l'un de ses sels, dans des conditions acides dans un milieu de réaction comprenant un mélange d'eau et d'un composé organique miscible avec l'eau.

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