Method for producing acylated peptides

Abstract From the Canadian patent

The present invention provides a method for acylating one or more amino groups of a peptide where the acylation reaction is to be performed in an aqueous mixture containing less than 10 %w/w aprotic polar solvent. a) reacting the peptide having at least one free amino group with an acylating agent of the general formula I wherein n, is 0-8 R1is COOR4; R2 is a lipophilic moiety; R3 together with the carboxyl group to which R3 is attached designate a reactive ester or a reactive N-hydroxy imide ester; and R4 is selected from hydrogen C1-12-alkyl and benzyl, under basic conditions in an aqueous mixture;