New general strategy of dimerization of bioactive molecules

We describe a new way of obtaining dimeric structures based on intermolecular diketopiperazine formation. The bioactive substance to dimerize was first linked to a glycine moiety. Then a coupling step using DMAP in stoichiometric quantity resulted in the cyclization involving both C-terminal carboxylic functions and the amide nitrogen. This general strategy has been applied to peptide and non-peptide bioactive molecules.