Author/Authors :
Molteni، نويسنده , , Marco and Volonterio، نويسنده , , Alessandro and Fossati، نويسنده , , Giacomo and Lazzari، نويسنده , , Paolo and Zanda، نويسنده , , Matteo، نويسنده ,
Abstract :
The aza-Michael addition of amines and β-amino-alcohols to trifluorocrotonic acid derivatives is described. The reactions occurred in good to excellent yields, but low stereocontrol. The title reaction has been used as a key step for the synthesis of trifluoroethylamine mimics of retro-thiorphan, which showed low inhibitory activity of NEP (constant inhibition at the molar level).
