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Functionalized methylenediphosphonic acids and their derivatives with aromatic and heterocyclic moieties are well-known biomimetics of hydroxy- or aminocarboxylic acids and natural pyrophosphates, and some of them such as zoledronic, risedronic, and minodronic acids are widely used in medicine. Organosilicon-mediated synthesis of functionalized organophosphorus acids and their derivatives was used recently by us as convenient method of creating of P-C bonds. We have synthesized the new functionalized methylenediphosphonic acids and their derivatives 1 including aromatic, azaheterocyclic, and amino acids moieties via addition of tris(trimethylsilyl) phosphite to corresponding formamides.The resulting compounds are the perspective biologically active substances and polydentate ligands with versatile properties as well as the promising precursors for multitarget drug discovery.This work was financially supported by the RFBR (grant number 17-03-00169).