Abstract
α-Benzylphenylalanine is best prepared by use of the Ugi four-component condensation method, followed by hydrolysis and hydrogenolysis of the intermediate N-acetyl-N,α-dibenzylphenylalanine. The same general procedure gives good yields of α-benzylphenylalanine peptides, but is limited in its application owing to the complete racemisation which attends the conversion of L-amino-acid esters into the isocyanides. The oxazolinone method is useful for the synthesis of peptides of α-benzylphenylalanine by the fragment condensation strategy employing small peptides containing C-terminal α-benzylphenylalanine residues, but breaks down with larger peptides. Many, but not all, derivatives of α-benzylphenylalanine show magnetic non-equivalence of the benzyl methylene protons.

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