ИСТИНА

The convenient synthesis of new functionalized aryl and hetaryl amino-methylenebisphosphonic acids has been developed via silicon-assisted methodology. New functionalized aminomethylenebisphosphonic acids containing aryl, pyridine and quinoline moieties were obtained using unique reaction of tris(trimethylsilyl) phosphite with N-formyl derivatives of corresponding (het)arylamines and trimethylsilyl triflate as a catalyst under mild conditions. Intermediates – tetra(trimethylsilyl) aminomethylenebisphosphonates formed, were converted to the target acids by further treatment with methanol excess. The catalytic schemes of target substances formation are proposed.