Enzymic synthesis design and enzymic synthesis of aspartame

Article abstract of DOI:10.1016/S0040-4020(01)88207-7

An enzymic synthesis of aspartame (H-Asp-Phe-OMe) has been designed and realized based on the structure-activity study of thermolysin and penicillin amidase hydrolysis of its p-substituted phenylacetyl derivatives. These compounds meet the structural and energetic requirements of two enzymic binding sites. The peptide sweetener has been prepared by thermolysin - catalyzed condensation of the p-substituted phenylacetyl-Asp-OH and H-Phe-OMe follwed by penicillin amidase - catalyzed deprotection of the resulted aspartame precursors.