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AssigneeNippon Kayaku Kabushiki Kaisha
InventorsTadashi Fujii, Hiroshi Yagiuchi, Akikazu Mitsunobu, Shigeru Aoki, Makoto Tsuda
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The present invention relates to a process for producing .alpha.-aspartyl-phenylalanine ester represented by the general formula ##STR1## wherein R' represents an alkyl group having 1 to 4 carbon atoms, by reducing an N-protected-N-hydroxymethyl-.alpha.-aspartyl-phenylalanine ester represented by the general formula ##STR2## wherein R represents an organic mioety which can be substituted reductively by hydrogen, and R' is as defined above, with hydrogen gas or formic acid, in the presence of a reduction catalyst and an aromatic primary amine. According to the present invention, there can be obtained a high purity .alpha.-aspartyl-phenylalanine ester with a high yield.
A process for producing .alpha.-aspartyl-phenylalanine ester represented by the general formula (I) ##STR10## wherein R' represents an alkyl group having 1 to 4 carbon atoms, which comprises reducing an N-protected-N-hydroxymethyl-.alpha.-aspartyl-phenylalanine ester represented by the general formula (IV) ##STR11## wherein R represents an organic moiety which can be substituted by hydrogen reductively, and R' is as defined above, with hydrogen gas or formic acid in the presence of a reduction catalyst and an aromatic primary amine.
A process for producing .alpha.-aspartyl-phenylalanine lower alkyl ester which comprises reducing N-benzyloxycarbonyl-N-hydroxymethyl-.alpha.-aspartyl-phenylalanine lower alkyl ester with hydrogen gas in a mixed solvent of water and a lower alcohol in the presence of palladium-carbon and aniline.
A process for producing .alpha.-aspartyl-phenylalanine lower alkyl ester which comprises reducing N-benzyloxycarbonyl-N-hydroxymethyl-.alpha.-aspartyl-phenylalanine lower alkyl ester with formic acid in a mixed solvent of water and a lower alcohol in the presence of palladium-carbon and aniline.
Dependencies are inferred from the claim text.