Synthesis of 3,5-Disubstituted Piperazinones via Palladium(II)-Catalyzed Amination

Abstract
The synthesis of 3,5-disubstituted piperazinones has been achieved in quantitative yields via an intramolecular palladium(II)-catalyzed allylic amination in the presence of LiCl and without a reoxidizing system. These conditions, that allow higher diastereoselectivities than those reported earlier using Pd(0), are associated to a different and irreversible process. Conveniently, the stereoselectivity is reversed if the reaction is performed in the absence of LiCl.

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