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Review | Regular issue | Vol 91, No. 7, 2015, pp.1349-1375
Published online, 14th May, 2015
DOI: 10.3987/REV-15-820
Chemistry of 2,5-Diketopiperazine and Its Bis-Lactim Ether: A Brief Review

Shigeki Sano* and Michiyasu Nakao

*Molecular Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, The University of Tokushima, 1-78 Sho-machi, Tokushima 770-8505, Japan


2,5-Diketopiperazines have attracted much attention because of their biological activities and molecular structure characteristics. Bis-lactim ethers derived from these 2,5-diketopiperazines include well-known organic molecules such as Schöllkopf chiral auxiliaries, which are used in asymmetric synthesis of α-amino acids. In this article, we briefly discuss the chemistry of both heterocyclic compounds.