3-amino-2-piperidones as constrained pseudopeptides: Preparation of a new Ser-Leu surrogate

Article abstract of DOI:10.1016/S0040-4039(99)00897-7

We describe a stereoselective preparation of 3-amino-2-piperidone 1, a new conformationally constrained Ser-Leu surrogate. The key steps of the synthesis of compound I are the lactamisation of the secondary aminolactone 4 and the amination of the 3-position via the sulfite 2.