Regio- and Diastereoselective Construction of α‑Hydroxy-δ-amino Ester Derivatives via 1,4-Conjugate Addition of β,γ-Unsaturated N‑Sulfonylimines

A first example of 1,4-conjugate addition of β,γ-unsaturated N-sulfonylimines via the oxonium ylides trapping process was developed. This method afforded a novel and efficient access for the high regio- and diastereoselective construction of α-hydroxyl-δ-amino esters derivatives, which exhibit inhibitory activity on PTP1B and SIRT1 enzymes in vitro. The synthetic potentials and the biological activity of the resulting products were well demonstrated to be promising for drug discovery.