Síntesis de monosuccinato de solifenacina

Un método para producir succinato de solifenacina, que comprende permitir que reaccione ácido succínico con un compuesto representado por una fórmula (II) [en la fórmula, la estereoquímica de la posición 1 de la tetrahidroisoquinolina sustituida con fenilo es una mezcla de la forma (R) y la forma (S) ], en el que el compuesto representado por la fórmula (II) es (3R) -quinuclidin-3-il éster del ácido (1RS) -1-fenil-1, 2, 3, 4tetrahidroisoquinolin-2-carboxílico. 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.