PROCESS FOR MAKING PEPTIDES CONTAINING AZA-AMINO ACIDS

摘要

A process for the solid phase synthesis of peptides containing a C-terminal aza-amino acid, for example the decapeptide goserelin, which comprises: (i) reacting an active ester or imidazolide of an N-protected aza-amino acid either with an appropriate reactive solid support in the case of the synthesis of a peptide containing a C-terminal aza-amino acid, or with a peptide which is attached to a solid support in the case of the synthesis of a peptide containing a non-C-terminal aza-amino acid; (ii) carrying out further conventional solid phase peptide synthesis steps to add sequentially further amino acids, to form a peptide with the required amino acid sequence bound to the solid support; (iii) cleaving the peptide from the solid support, and optionally (iv) reacting the product so formed with hydrazine to remove any acyl groups which have been formed on serine, arginine, tyrosine, threonine or hydroxyproline during the synthesis.