Two novel metabolites have been isolated from the aerial parts of Stachys ehrenberiigii. Their structures and stereochemistry were elucidated using a combination of 13C and 1 H homo and heteronuclear 2D NMR experiments and mass analysis. The development of an enantioselective synthesis of 3-(20 -acetoxy-4-phenylbut-30 -enoylamino)propionic acid allowed to confirm the structure and assign the (R) absolute configuration at C-20 of the natural product.