Process for producing .alpha.-L-aspartyl-L-phenylalanine methyl

Organic compounds -- part of the class 532-570 series – Organic compounds – Carboxylic acid esters

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560 41, C07C22900

Patent

active

053347463

ABSTRACT:
A process for the preparation of .alpha.-L-aspartyl-L-phenylalanine methyl ester in high yield, which comprises the steps of esterifying L-phenylalanine with methanol while undergoing continuous evaporation to remove the water formed during esterification, coupling the produced L-phenylalanine methyl ester with N-formyl-L-aspartic anhydride, deformylating the produced N-formyl-L-aspartyl-L-phenylalanine methyl ester, crystallizing the formed .alpha.-L-aspartyl-L-phenylalanine methyl ester as .alpha.-L-aspartyl-L-phenylalanine methyl ester hydrochloric acid salt, recovering the first .alpha.-L-aspartyl-L-phenylalanine methyl ester hydrochloric acid salt, esterifying .alpha.-L-aspartyl-L-phenylalanine in the filtrate to produce the second .alpha.-L-aspartyl-L-phenylalanine methyl ester, and combining the first and second .alpha.-L-aspartyl-L-phenylalanine methyl ester product.

REFERENCES:
patent: 3492131 (1970-01-01), Schlarter
patent: 3786039 (1974-01-01), Ariyoshi et al.
patent: 4071511 (1978-01-01), Takemoto et al.
patent: 4680403 (1987-07-01), Hisamitsu et al.
patent: 4684745 (1987-08-01), Takemoto et al.
patent: 4760164 (1988-07-01), Park et al.

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