Multistep Synthesis of 2,5-Diketopiperazines on …

AB - 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.

Efficient synthesis of 2,5-diketopiperazines by Staudinger-mediated cyclization.

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.


The nonribosomal synthesis of diketopiperazines in …

In particular novel diketopiperazines are disclosed including their synthesis and use in cellular events such as activation of the transcription factor, nuclear factor, TNF-alpha, TNF-beta and also apoptosis.