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The condensation of tris(trimethylsilyl) phosphite with various ketimines leads directly to tetrasubstituted αaminophosphonic acids. The presented reaction proceeds readily at room temperature and provides labile silylated esters of tetrasubstituted α-aminophosphonic acids, as non-isolable reaction intermediates. Subsequent methanolysis of the latter provides the desired α-aminophosphonic acids bearing an fully substituted α-carbon in good overall yields as crystalline non-hygroscopic solids after simple recrystallization from a methanol-acetone mixture.nordstom

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Application of tris(trimethylsilyl) phosphite as convenient phosphorus nucleophile in the direct synthesis of tetrasubstituted α-aminophosphonic acids from ketimines