L-Aspartic Acid → L-Phenylalanine, methyl ester

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Reaction Steps

Accordingly, this invention provide a process for producing an addition compound of a dipeptide ester and an amino acid ester, in which aspartic acid and benzyloxycarbonyl chloride is reacted in an aqueous solution in the presence of a base to prepare a solution containing N-benzyloxycarbonyl aspartic acid; phenylalanine and methanol are separatedly reacted in the presence of an acid to produce phenylalanine methyl ester; excess methanol is substituted with water to convert it to an aqueous solution of phenylalanine methyl ester; it is admixed with the above-prepared aqueous solution containing N-benzyloxycarbonyl aspartic acid; an proteolytic enzyme is added into the resulting mixture under conditions, under which no substantial deactivation of the enzyme occurrs; N-benzyloxycarbonyl aspartic acid and phenylalanine methyl ester are reacted under conditions, under which the proteolytic enzyme exerts the enzymatic activity, to deposit an addition compound of N-benzyloxycarbonyl-α-L-aspartyl-L-phenylalanine methyl ester and phenylalanine methyl ester; and then the addition compound is recovered.

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