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Potassium Carbonate Catalyzed Intramolecular Post-Ugi Hydroamination Reaction Leading to N -Aryl Piperazine Derivatives Publisher



Yazzaf R1 ; Sayahi MH2 ; Mahdavi M3
Authors

Source: Synlett Published:2025


Abstract

N -Arylpiperazines are prominent structures found in natural products and synthetic chemical entities, including therapeutic agents. In this work, we introduce a novel strategy for the effective synthesis of distinctive piperazine compounds through a post-Ugi cyclization under transition-metal-free conditions. This method involves the formation of a four-component Ugi adduct by combining an aldehyde, an isocyanide, a primary propargylamine, and an oxamic acid. Subsequently, an intramolecular alkyne hydroamination reaction occurs, leading to the formation of a piperazine derivative through carbon-nitrogen bond formation. The products have been characterized by 1 H and 13 C NMR spectroscopy. © 2025 Georg Thieme Verlag. All rights reserved.
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