The Mitsunobu reaction has been used as an efficient tool for the synthesis of orthogonallyprotected and unprotected depsipeptides such as Boc/Fmoc-l-Lys(Alloc)-d-Ala-d-Lac-OAllyl or l-Lysd-Ala-d-Lac that are bacterial cell wall precursor analogues found in vancomycin-resistant enterococci.