Improved process for the preparation of entacapone

Details Improved process for the preparation of entacapone Improved process for the preparation of entacapone

C - Chemistry, Metallurgy

07

C

C07C 255/41 (2006.01) C07C 253/30 (2006.01)

Patent

CA 2552099

The invention disclosed in this application relates to an improved process for the preparation of the Entacapone which comprises. (i)reacting 3-alkoxy- 4- hydroxy-5-nitrobenzadehyde with N,N-diethylaminocyanoactamide in the presence of mild acid catalyst and a solvent at a temperature in the range of 50-115 ~C, to get the 3-O-alkylated (methyl or ethyl) Entacapone and treating with acid catalysts in the presence of organic base and solvents at temperature in the range of 20-60 ~C to get Entacapone.

cette invention concerne un procédé amélioré permettant de préparer de l'entacapone, lequel procédé consiste (i) à faire réagir 3-alkoxy-4-hydroxy-5-nitrobenzadéhyde avec N,N-diéthylaminocyanoactamide en présence d'un catalyseur acide doux et d'un solvant à une température comprise entre 50 et 115 ·C, pour obtenir l'entacapone 3-O-alkylaté (méthyl ou éthyl), puis à traiter avec des catalyseurs acides doux en présence d'une base organique et de solvants à une température comprise entre 20 et 60 ·C pour obtenir l'entacapone.

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