The new functionalized aminomethylenediphosphonates with moieties of various amino acids are synthesized via unique reaction of tris(trimethylsilyl) phosphite and N-formyl amino acids at the presence of effective catalyst – trimethylsilyl triflate under mild conditions. The further treatment of aminomethylenediphosphonates with the methanol excess resulted in the water-soluble functionalized aminomethylenediphosphonic acids.