Process for the preparation of zaleplon

C - Chemistry – Metallurgy – 07 – D

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C07D 487/04 (2006.01) C07D 231/00 (2006.01) C07D 239/00 (2006.01)

Patent

CA 2503152

N-[3-(3-Dimethylamino-acryloyl)-phenyl]-N-ethyl-acetamide is reacted with 5- ~amino- lH-pyrazol-4-carbonitrile in a medium comprising a solution of hydrochloric or hydrobromic acid in a C1-C5 alcohol, or in a C4-C6 aliphatic or cyclic ether, or in a C2-C5 alkoxyalcohol, or in a 5- to 6-membered aromatic heterocyclic solvent, containing 1-2 oxygen atoms, or in mixtures thereof with water, thus forming ZALEPLON.

Selon la présente invention, on fait réagir un <I>N</I>-[3-(3-Diméthylamino-acryloyl)-phényl]-<I>N</I>-éthyl-acétamide avec un 5-amino-1<I>H</I>-pyrazol-4-carbonitrile dans un milieu comprenant une solution d'acide hydrochlorique ou hydrobromique dans un alcool C1-C5, ou dans un éther cyclique ou aliphatique C4-C6, ou dans un alcoxyalcool C2-C5, ou dans un solvant hétérocyclique aromatique à 5 ou 6 chaînons contenant de 1 à 2 atomes d'oxygène, ou dans des mélanges de ces derniers avec de l'eau, afin de former du ZALEPLON.

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