KR890016005A - Method for preparing alanine derivative - Google Patents

Abstract

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Description

Method for preparing alanine derivative

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Claims (7)

A first step of preparing an amine compound of formula (IV) by reacting an amino derivative of formula (II) and a propionic acid derivative of formula (III) with an organic solvent and a base, and an amine compound of formula (IV) and general A process for producing an alanine derivative of formula (I), characterized by comprising a second step of producing alanine derivative of formula (I) by reacting a proline derivative of formula (V) in an aqueous alkali solution. In general formula (I), R <^1> represents a phenyl group, R <^2> is an ethyl group, R <^3> represents hydrogen R <^4> hydrogen, and R <^5> represents hydrogen or benzyl group, respectively. In the formula (Ⅱ), R ¹ is a phenyl group, R ² is an ethyl group and R ^× denotes a hydrogen, respectively. In formula (III), R ⁵ represents hydrogen or benzyl group and X represents bromine or chlorine. In general formula (IV), R <^1> represents a phenyl group, R <^2> is an ethyl group, R <^3> is hydrogen, and R <^5> represents a hydrogen or benzyl group, respectively. R ⁴ in General Formula (V) represents hydrogen. The process for producing an alanine derivative of the general formula (I) according to claim 1, wherein dimethylformamide or chloroform is used as the organic solvent. The process for producing an alanine derivative of formula (I) according to claim 1, wherein triethylamine or trimethylamine is used as a base. The process for producing an alanine derivative of formula (I) according to claim 1, wherein the reaction temperature is reacted at 20-30 占 폚. The method for producing an alanine derivative of the general formula (I) according to claim 2, wherein sodium bicarbonate is used as the alkali. The process for producing an alanine derivative of formula (I) according to claim 2, wherein the reaction is carried out at a reaction temperature of 20-30 캜. In the second process of claim 1, in order to improve maleate salt of the alanine derivative of general formula (I), N (1-ethoxycarbonyl-3-phenylpropyl) -alanyl- (S) -proline A maleic acid is added in a molar ratio of 1: 1, and selected from ethyl acetate, acetonitrile and acetone to dissolve to produce maleic acid salt of the alanine derivative of formula (I). ※ Note: The disclosure is based on the initial application.