CHEMICAL PROCESS FOR THE SELECTIVE MODIFICATION OF PEPTIDES

摘要

Method for selective modification of a peptide of general formula (30) to obtain a peptide of general formula (31) where [aa]n represents the N-terminal end of the peptide with a variable number n of amino acids, [aa]m represents the C-terminal end with a variable number m of amino acids, and the sum of m + n is an integer between 1 and 50, Y is chosen from -CH2-, -CH(alkyl)- and -C(=0)-, Z is chosen from hydrogen or an amine-protecting group, and [A]¡ is chosen from groups in which A represents CH2, a substituted carbon or a heteroatom, and i represents an integer between 1 and 10; characterized in that said method comprises the steps of [a] oxidative radical cleavage of the peptide of general formula (30), and [b] addition of a carbon nucleophile to the imine intermediate formed in order to obtain a peptide of general formula (31). The invention also relates to the peptides of formula (31) obtained by means of this method and peptides derived therefrom.