Preparation process of .alpha.-L-aspartyl-L-phenylalanine methyl

Details Preparation process of .alpha.-L-aspartyl-L-phenylalanine methyl Preparation process of .alpha.-L-aspartyl-L-phenylalanine methyl

1987-11-17

1988-10-18

Kight, John

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acid esters

560 41, 530801, 426548, C07C10352, C07C10200

Patent

active

047789166

ABSTRACT:
The present invention relates to a process for preparing .alpha.-L-aspartyl-L-phenylalanine methyl ester or its hydrochloride. .alpha.-L-aspartyl-L-phenylalanine methyl ester or its hydrochloride is prepared by a process comprising: condensating N-formyl-L-aspartic acid anhydride and L-phenylalanine in water or in water containing methanol at a pH in the range of 7-12 to form N-formyl-.alpha.-L-aspartyl-L-phenylalanine; acidifying the reaction mixture successively with hydrochloric acid in the presence of methanol without isolating the N-formyl-.alpha.-L-aspartyl-L-phenylalanine so as to bring it into contact with hydrochloric acid in the presence of methanol for reaction and thereby to deposit .alpha.-L-aspartyl-L-phenylalanine methyl ester hydrochloride; separating the .alpha.-L-aspartyl-L-phenylalanine methyl ester hydrochloride; and neutralizing said hydrochloride as required.

REFERENCES:
patent: 3879372 (1975-04-01), Boesten
patent: 3933781 (1976-01-01), Bachman et al.
patent: 4021418 (1977-05-01), Takemoto et al.
patent: 4071511 (1978-01-01), Takemoto et al.
patent: 4088649 (1978-05-01), Smith et al.
patent: 4153737 (1979-05-01), Berg et al.
patent: 4579747 (1986-04-01), Sugiyama et al.
patent: 4634790 (1987-01-01), Shinohara et al.
Chemical Abstracts, 105:153551s.

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