Expedient synthesis of novel bicyclic peptidomimetic scaffolds

In the past, bicyclic structures mimicking dipeptides have been designed and successfully used to prepare enzyme inhibitors. We report herein our preliminary results in the design and expedient synthesis of a novel series of diastereomeric N-amino-hexahydro-1H-isoindolone scaffolds built from three commercially available building blocks in only two steps, with high yields, a single protecting group and a single purification step.