Method for producing solifenacin or salts thereof

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 453/02 (2006.01)

Patent

CA 2564757

There is provided a novel method for producing solifenacin or a salt thereof which is useful as a medicine, particularly a therapeutic agent and/or a preventive agent for a urinary organ system disease such as pollakiuria or urinary incontinence. Illustratively, there are provided (1) a method for producing solifenacin in which 2-(1H-imidazolylcarbonyl)-1- phenyltetrahydroisoquinoline is used as the starting material, (2) a method for producing solifenacin succinate in which (1RS)-phenyltetrahydroisoquinoline-carboxylic acid quinuclidinyl ester is used as the starting material, (3) a method for producing solifenacin in which a lower alkyl quinuclidinyl carbonate is used as the starting material and (4) a method for producing solifenacin in which phenyltetrahydroisoquinoline-carboxylic acid secondary lower alkyl or tertiary lower alkyl ester is used as the starting material and allowed to react with an alkali metal lower alkoxide.

Nouveau procédé servant à produire de la solifénacine ou son sel qui est utile comme médicament, en particulier comme agent thérapeutique et/ou préventif pour des maladies urinaires, telles que la miction fréquente et la miction involontaire. En particulier, il est fourni (1) un procédé servant à produire de la solifénacine à partir de 2-(imidazolylcarbonyl)-1-phényltétrahydroisoquinoline servant de matière de départ pour la production ; (2) un procédé servant à produire du succinate de solifénacine à partir de (1RS)-phényltétrahydroisoquinolinecarboxylate de quinuclidinyle servant de matière de départ pour la production ; (3) un procédé servant à produire de la solifénacine à partir d'un carbonate d'(alkyle inférieur)quinuclidinyle servant de matière de départ pour la production ; et (4) un procédé servant à produire de la solifénacine, comprenant de faire en sorte qu'un alcoxyde inférieur de métal alcalin agisse sur un phényltétrahydroisoquinolinecarboxylate d'alkyle inférieur secondaire ou d'alkyle inférieur tertiaire servant de matière de départ pour la production.

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