N-3, 3-dimethylbutyl-l-aspartic acid and esters thereof, the process of preparing the same, and the process for preparing n-(n-(3, 3-dimenthylbutyl)-l-alpha-aspartyl)-l-phenylalanine 1-methyl ester therefrom

摘要

This invention relates to the chemical synthesis of N-[N-(3,3-dimethylbutyl)-L- alpha -aspartyl]-L-phenylalanine 1-methyl ester using peptide coupling methods. The coupling reaction is conducted by condensation of an activated derivative of novel N-neohexyl-L-aspartic acid with L-phenylalanine or L-phenylalanine methyl ester or by enzymatic coupling of N-neohexyl-L-aspartic acid with L-phenylalanine or L-phenylalanine methyl ester. This invention also relates to novel N-(3,3-dimethylbutyl)-L-aspartic acid, derivatives thereof and the preparation thereof. The activated derivative of N-neohexyl-L-aspartic acid may be an anhydride, mixed anhydride, active ester or an intermediate activated derivative thereof.