A process for selectively esterifying. alpha. -L-aspartyl-L-phenylalanine to the corresponding alkyl esters using a proteolytic enzyme with specific esterase activity is described. The process is carried out in an aqueous-alcohol medium in which the alcohol concentration is sufficient to reverse the esterase activity. The. alpha. -L-aspartyl-L-phenylalanine alkyl esters so produced are useful as artificial sweeteners.
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