Condensation method in production process of N-alpha-L-aspartyl-L-phenylalanine 1-methyl ester

Abstract

The invention discloses a condensation method in a production process of N-alpha-L-aspartyl-L-phenylalanine 1-methyl ester. The condensation method comprises the steps of: adding N-formyl-alpha-L-aspartic anhydride into a mixture of L-phenylalanine, water and sodium hydroxide; carrying out a reaction; adjusting the PH value; and carrying out separation to obtain the N-alpha-L-aspartyl-L-phenylalanine 1-methyl ester. The condensation method in the production process of N-alpha-L-aspartyl-L-phenylalanine 1-methyl ester disclosed by the invention greatly improves the yield of N-alpha-L-aspartyl-L-phenylalanine 1-methyl ester and effectively controls racemization of L-phenylalanine in a production process.

Description

technical field [0001] The invention belongs to the field of chemical industry, and in particular relates to a condensation method in the production process of N-α-L-aspartate-L-phenylalanine 1-methyl ester. Background technique [0002] N-α-L-aspartame-L-phenylalanine 1-methyl ester (C 14 h 18 N 2 o 5 ), commonly known as aspartame, is a non-carbohydrate artificial sweetener with poor thermal stability, relatively stable below 55°C, relatively stable between pH 2 and 4, and its hydrochloride High solubility. [0003] N-α-L-aspartame-L-phenylalanine 1-methyl ester (C 14 h 18 N 2 o 5 ) is rapidly metabolized into aspartic acid, phenylalanine and methanol in the body. Even with high intake of N-α-L-aspartate-L-phenylalanine-methyl ester (C 14 h 18 N 2 o 5 ) (200 mg per kg body weight), aspartame could not be detected in the blood. [0004] From N-α-L-aspartate-L-phenylalanine 1-methyl ester (C 14 h 18 N 2 o 5 ) provides only 1-2% of the body's daily intake of...

AI Technical Summary

Problems solved by technology

[0008] In the existing condensation process, the racemization of the raw material L-phenylalanine is serious, the consumption of N-formyl-α-L-aspartic anhydride is large, the reaction of L-phenylalanine is incomplete, and the overall recovery The rate is low, and the obtained product a body (N-formyl-α-L-aspartyl-L-phenylalanine) and its stereoisomer b body (N-formyl-β-L-day Partyine-L-phenylalanine) has large fluctuations in the production ratio, high energy consumption and other adverse production effects