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An efficient two-step multigram synthesis of the previously unknown 3-benzyl-3-azabicyclo[3.1.1]heptan-6-one is described. The compound is shown to be a promising building block for further selective derivatization of the cyclobutane ring providing novel conformationally restricted piperidine derivatives.

3-Benzyl-3-azabicyclo[3.1.1]heptan-6-one: A Promising Building Block for Medicinal Chemistry