Solid-phase synthesis of diketopiperazines, useful scaffolds for combinatorial chemistry

Abstract

Diketopiperazines, which are cyclic dipeptides, are often formed by a side reaction of solid-phase peptide synthesis. Using the new 'Backbone Amide Linker,' this chemistry can be conveniently harnessed for the intentional preparation of diketopiperazines. These products will be useful scaffolds for combinatorial chemistry, since they incorporate three different points of diversity: both amine acid side-chains and one (of the two) amide bonds.