Synthesis of N-[N-(3,3-dimethylbutyl)-L-alpha-aspartyl]-L-phenylalanine 1-methyl ester using L-alpha-aspartyl-L-phenylalanine 1-methyl ester precursors

摘要

N-(N-(3,3-Dimethylbutyl)-L-alpha -aspartyl)-L phenylalanine 1-methyl ester (neotame) is prepared using L-alpha aspartyl-L-phenylalanine 1-methyl ester (aspartame) precursors, without isolation of aspartame. Preparation of N-(N-(3,3 dimethylbutyl)-L-alpha -aspartyl)-L-phenylalanine 1-methyl ester of formula (I) comprises reacting an acid salt of L-alpha -aspartyl-L-phenylalanine 1-methyl ester of formula (II), or N-protected-L-alpha -aspartyl-Lphenylalanine, with 3,3-dimethylbutyraldehyde of formula (III) in a solvent in the presence of a catalyst and hydrogen to give (I). [Image].