Improved process for the preparation of rivastigmine

Details Improved process for the preparation of rivastigmine Improved process for the preparation of rivastigmine

C - Chemistry, Metallurgy

07

C

C07C 215/50 (2006.01) C07C 269/04 (2006.01) C07C 271/44 (2006.01)

Patent

CA 2661009

The present invention relates to an improved process for preparation of Rivastigmine of formula (I) or pharmaceutically acceptable salts thereof comprising a step of N-methylation of compound of formula (III), wherein R1 = R2 = H or R1 = H and R2 = CH3 or an acid addition salt thereof, using paraformaldehyde in the presence of Raney Nickel and hydrogen in a suitable solvent to obtain compound of formula (II).

La présente invention concerne un procédé perfectionné pour la préparation de Rivastigmine de formule (I) ou de ses sels pharmaceutiquement acceptables, ledit procédé comportant une étape de N-méthylation du composé de formule (III) dans laquelle R1 = R2 = H ou R1 = H et R2 = CH3 ou un sel d'addition avec un acide de celui-ci grâce à du paraformaldéhyde en présence de Nickel de Raney et d'hydrogène dans un solvant approprié pour obtenir un composé de formule (II).

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