Diastereoselective Synthesis of the Hydroxyethylene Dipeptide Isostere of Leu–Val

Abstract
The synthesis of hydroxyethylene dipeptide isostere of Leu–Val, a transition-state mimic, is described. The key steps of this synthetic approach are the homogeneous asymmetric hydrogenation of γ-keto esters by BINAP–Ru(II) complex, and the construction of a 2(S)-isopropyl unit.