New bioorganometallic ferrocene derivatives are synthesized through a Diversity Oriented Synthesis strategy. Easily available ferrocene bisimines have been transformed into open ferrocenyl bis-β-lactams. These compounds have demonstrated to be versatile synthons used in further transformations into new ferrocene bis-β-amino acids. Carefully selected substituents submitted to ring closing metathesis (RCM) and Cu-catalyzed oxidative alkyne coupling conditions have also allowed the conversion of open substrates into ferrocenic macrocyclic bis-β-lactams.