A general method for the construction of diazepinone and homopiperazine scaffolds has been developed by utilizing Beckmann rearrangement as the key step in the design. Using this methodology, the synthesis of a diverse diazepinone library with three points of diversity has been achieved starting from readily available 4-piperidone.
Keywords: signal transduction, g-protein coupled receptors, piperazines, piperidines
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