Piperazin-2-one and 1, 4-diazepan-2-one scaffolds are featured in biologically active natural products and pharmaceutical compounds,[1] such as peptidomimetics,[2] compounds with potential to reverse multi-drug resistance in cancer treatments (ardeemins),[3] antibiotics (caprazamicins),[4] sedatives, and tranquilizers (diazepam)[5]. These structures have therefore attracted considerable attention as important pharmacophores in the field of ...