SYNTHESIS OF p‐AMINO‐L‐PHENYLALANINE DERIVATIVES WITH PROTECTED p‐AMINO GROUP FOR PREPARATION OF p‐AZIDO‐L‐PHENYLALANINE PEPTIDES

Abstract
For affinity labeling of peptide hormone receptors, the use of peptides containing p-azidophenylalanine is desired. For the synthesis of p-azidophenylalanine peptides, the p-amino group of p-amino-L-phenylalanine is protected with the Z- or Boc residue via the Cu complex or by specific acylation at pH 4.6. The .alpha.-amino or .alpha.-carboxy group is blocked by a protecting group (Boc [butoxycarbonyl], Ddz [3,5-dimethoxy-.alpha.,.alpha.-dimethylbenzyloxycarbonyl], OMe, respectively, Z [benzyloxycarbonyl], Nps [p-nitrophenylthio], Ddz), which can be removed selectively. The synthesis of 9 derivatives of p-amino-L-phenylalanine for incorporation into the peptide chain is described. The p-amino-phenylalanine is converted to p-azidophenyalanine without affecting disulfide bridges.

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