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-α-ASPARTYL-L-PHENYLALANINE 1-METHYL ESTER THEREFROM

摘要

This invention relates to the chemical synthesis of N-[N-(3,3-dimethylbutyl)-L-α-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-phenylalaline or L-phenylalanine methyl ester or by enzymatic coupling of N-neohexyl-L-aspartic acid with L-phenylalaline 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.