Ugi-4CR/S_N2-Cyclization Strategy for the One-Pot Synthesis of 2,5-Diketopiperazines

Abstract

2,5-diketopiperazines (2,5-DKPs) are the smallest cyclic peptides in nature and display a variety of antibacterial, antifungal, and anticancer properties. Very little has been reported on the one-pot synthesis of 2,5-DKPs. Herein, we report a novel one-pot synthesis of 2,5-DKPs via the Ugi-4CR/SN2-cyclization strategy, under mild conditions, and ethanol was used as a solvent for both procedures.

Keywords

• 2,5-DKPs
• IMCR
• Ugi-4CR
• bis-amide