Synthesis of 2‐(aminophenyl)‐2‐hydroxyethylphosphonates and their incorporation in short peptides

The synthesis of 2‐(Aminophenyl)‐2‐hydroxyethylphosphonates rac‐4a‐c is based on the formation of a hydroxyl function via addition of the lithium salt of dimethyl methylphosphonate (2) to aldehydes 1a‐c. The amino function in rac‐ 4a‐c is obtained by catalytic reduction of the nitro group in 3 at low pressure. The incorporation of the aminophosphonates rac‐4a‐c in short peptides, enables the formation of potential bioactive materials 12–14.