KR860001111A - Method for preparing amino eburnan carboxylic acid derivative - Google Patents

Abstract

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Description

Method for preparing amino eburnan carboxylic acid derivative

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Claims (2)

General obtained by the hydrolysis of the racemized or optically active 9- or 11-aminoebornanecarboxylic acid derivatives of the general formula (II) Wherein R represents a —NH—COR ¹ group or —NH—SO ₂ —R ² group (wherein R ¹ is a hydrogen atom, optionally substituted is the same as defined above), and A represents represents a hydroxyl group, B is a hydrogen atom, C ₁ ~ C ₁₀ aliphatic groups, C ₃ ~ C ⁸ cycloaliphatic or C _{6 ~ 14} aromatic, C _{6 ~ 14} hydrocarbyl group, or means a heterocyclic aromatic group, and R ² is an optionally substituted C _{1 ~ 10} aliphatic or C _{6 ~ 14} aromatic, C _{6 ~ 14} represent a hydrocarbyl group) represents; R ³ and R ⁴ are the same and A and B are the same as defined in the following general formula (I).] Ester or trans esterification of 9- or 11-aminoebunancarboxylic acid derivative of If necessary, General Formula (I) [wherein R represents a —NH—COR ¹ group or a —NH—SO ₂ R ² group (wherein R ¹ is the same as defined above), and A represents a hydroxyl group. , B is a hydrogen atom R ³ is an optionally substituted C _{1 ~ 10} aliphatic, C _{3 ~ 8} cycloaliphatic or aromatic C _{6 ~ 14,} wherein hydrocarbyl represents an invoke. racemic or optically active in the US of 9] Or hydrolyze, primary esterify or transesterify, if necessary, the 11-aminoetherancarboxylic acid derivative, and if necessary, the general formula (I) in which R represents an amino group and R ³ represents an optionally substituted C _1-10 aliphatic, C _{3 ~ 8} cycloaliphatic or C _{6 ~ 14} aromatic, Represents a drocarbyl group, A represents a hydroxyl group, and B represents a hydrogen atom.] Required after hydrolysis of the racemized or optically active 9- or 11-aminoebornanecarboxylic acid derivative of Racemed or optically active 9- or 11 of general formula (I) thus obtained wherein R represents an amino group and R ³ , A and B are as defined in the following general formula (I). -If necessary, after acylating the aminoebornanecarboxylic acid derivative, general formula (I), where R and R ³ are the same as defined above, A represents a hydroxyl group, and B represents a hydrogen atom. Dehydrated racemic or optically active 9- or 11-aminoebornanecarboxylic acid derivatives of Formula (I), wherein R, R ³ , A and B are Same as the definition in formula (I). Formula 1, characterized in that the optically active 9- or 11-amido bournancarboxylic acid derivatives are converted to acid addition salts and / or quaternary salts and / or partitioned racemic products thus obtained. A novel racemized and optically active 9- and 11-aminoebuernakirumic acid derivative of (I) and a method for producing the salt thereof. [Wherein, R represents an amino group or a —NH—COR ¹ group or a —NH—SO ₂ —R ² group (wherein R ¹ and R ² are the same as defined above); R ³ is a hydrogen atom, an optionally substituted C _{1 ~ 10} aliphatic groups, C _{3 ~ 8} cycloaliphatic or C _{6 ~ 14} aromatic C _{6 ~ 14} represents a hydrocarbyl group; A represents a hydroxyl group; B represents a hydrogen atom; Or A and B together form a valent bond; Conditional on: When R represents an amino group or —NH—COR ¹ in which R ¹ is a methyl group at position 11, R ³ is different from a methyl group, A means a hydroxyl group and B represents a hydrogen atom; When R means an amino group R ³ is different from a hydrogen atom and A and B together form a valence bond. R ⁴ represents a methyl group, and when A and B together form a valence bond, it also represents a hydrogen atom.] A new racemized or optically active 9- of general formula (I) prepared using the method according to claim 1 wherein R, R ³ , A and B are as defined in claim 1. Or 11-aminoetherancarboxylic acid derivative or a pharmaceutically acceptable salt thereof as an active ingredient, which is mixed with a carrier and / or an additive commonly used in the pharmaceutical industry and converted into a pharmaceutical composition. Process for preparing pharmaceutical composition. ※ Note: The disclosure is based on the initial application.