Process for obtaining olopatadine and intermediates

Details Process for obtaining olopatadine and intermediates Process for obtaining olopatadine and intermediates

C - Chemistry, Metallurgy

07

D

C07D 313/12 (2006.01)

Patent

CA 2730955

Olopatadine can be obtained by means of a process comprising hydrolysis of a compound of general formula (II), wherein Y is OR1, wherein R1 is C1-C7 alkyl, C3-C7 cycloalkyl, aryl, arylalkyl, or heterocycle; or NR2R3, wherein R2 and R3, independently from each other, are C1- C7 alkyl, aryl, arylalkyl, or R2 and R3 together with the nitrogen atom to which they are bound form a heterocycle of 3 to 7 members, obtained by means of a process comprising reacting the corresponding ester or amide of 6,11-dihydro-11- oxodibenz[b,e]oxepin-2-acetic acid with a suitable Wittig reagent, in the presence of a base in a reaction medium comprising an organic solvent.

Selon linvention, il est possible dobtenir de l'olopatadine au moyen d'un procédé comprenant l'hydrolyse d'un composé de la formule générale (II), dans laquelle Y représente OR1, R1 représente alkyle en C1-C7, cycloalkyle en C3-C7, aryle, arylalkyle ou hétérocycle; ou NR2R3, où R2 et R3, indépendamment l'un de l'autre, représentent alkyle en C1-C7, aryle, arylalkyle, ou R2 et R3, conjointement avec l'atome d'azote auquel ils sont liés, forment un hétérocycle de 3 à 7 chaînons, ce composé ayant été obtenu au moyen d'un procédé comprenant la réaction de l'ester ou de l'amide correspondant de l'acide 6,11-dihydro-11-oxodibenz[b,e]oxépin-2-acétique avec un réactif de Wittig approprié, en présence d'une base, dans un milieu de réaction renfermant un solvant organique.

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