Amino acid amides react with diethyl oxalate and sodium ethoxide to yield 6-substituted piperazine-2,3,5-triones, which can be mono-alkylated at N4, bis-alkylated at N4 and C6, or tris-alkylated at N4, N1, and C6 under mild basic conditions; this provides access to i) a,a-disubstituted cyclic peptide derivatives; ii) constrained peptides via C(a)-N bond formation; iii) DKP analogues.
|Number of pages||4|
|Publication status||Published - 15 Oct 1999|
- Amino acids and derivatives
- Peptide analogues/mimetics