Synthesis of Piperazin-2-ones via Cascade Double Nucleophilic Substitution

Synthesis of Piperazin-2-one Derivatives via Cascade Double Nucleophilic Substitution: M. Petkovic, D. Kusljevic, M. Jovanovic, P. Jovanovic, G. Tasic, M. Simic, V. Savic
Synthesis 2023, DOI: 10.1055/a-2201-9951

Small heterocyclic rings are encountered in countless bioactive natural products and are extensively used as structural scaffolds in drug discovery or as bioisosteric replacements in biological chemistry to impart specific physicochemical/pharmacokinetic properties to drug candidates. Thus, synthetic chemists continue to focus their efforts on the development of novel strategies for the efficient and rapid synthesis of structurally varied small heterocycles. Recently, the group of Professor Vladimir Savic and Dr. Milos Petkovic from the University of Belgrade (Serbia) described a novel metal-promoted cascade approach to piperazin-2-ones, based on the use of a chloro allenylamide, primary amines, and aryl iodides as substrates.


Professor Savic said: “Efficiency of the methodology, introducing two points of diversity and creating three bonds in a single step, makes the described process a valuable synthetic tool for the preparation of biologically important 2-piperazinones either as individual derivatives or as combinatorial compound collection.” 

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