Efficient synthesis of substituted piperazinones via tandem reductive amination–cyclization

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A new strategy for the preparation of substituted piperazinones features a tandem reductive coupling and S N2-cyclization of a 2-chloro- N-(2-oxoalkyl)acetamide ( 1) and a primary amine ( 2). The method is convenient for diversity-oriented synthesis, since a wide variety of amines may be used in the ring-forming reaction to produce N-substituted piperazinones ( 3).