Author/Authors :
Volonterio، نويسنده , , Alessandro and Chiva، نويسنده , , Gema and Fustero، نويسنده , , Santos and Piera، نويسنده , , Julio and Sanchez Rosello، نويسنده , , Maria and Sani، نويسنده , , Monica and Zanda، نويسنده , , Matteo، نويسنده ,
Abstract :
N-Acylation of Wang resin-bound l-α-amino acids with 2-trifluoromethyl-propenoyl chloride, followed by asymmetric tandem aza-Michael/enolate-protonation by a series of l-α-amino esters and final release from the resin, afforded a representative library of partially-modified retropeptides incorporating a stereodefined trifluoroalanine surrogate. The stereocontrol can be dramatically improved (up to 15:1) by using apolar solvents like carbon tetrachloride and DABCO as base.
