Abstract

An extremely efficient synthesis of Δ 5-2-oxopiperazines in solution phase and on solid support has been established via a Ugi four-component condensation reaction (U-4CC) followed by N-acyliminium ion cyclization between the aldehyde (acetal) functionality and the newly formed amide bond. The desired Δ 5-2-oxopiperazines are obtained in excellent yields and purity.

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