Abstract

Diversity-oriented synthesis of 2, 5-diketopiperazines was accomplished via Ugi/aza-Michael reaction cascades in one pot. The intramolecular hydrogen bonding between the heteroatom (O or N) from the aldehyde component and the amide -NH group facilities the aza-Michael transformation. This protocol offers a straightforward and concise method to build diversified 2, 5-diketopiperazines library for drug discovery.

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