A simple and efficient one-pot three-component synthetic route to highly substituted and functionalizable piperazines in high yields with excellent stereoselectivity (de, ee >99%) is reported. The S2-type ring-opening of N-activated aziridines by anilines followed by Pd-catalyzed annulation with propargyl carbonates gives rise to the final piperazine products.

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http://dx.doi.org/10.1021/acs.joc.8b02259DOI Listing

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