Stereospecific Transformation of Protected P?H Group into P?O or P?N Group in One-Pot Reaction

摘要

A general and efficient procedure for converting 1,1-diethoxyalkylphosphinatesninto phosphonates or phosphonamides is described by thenapplication of bromine with moderate to high yields and good purity in a onepotnreaction. H-Phosphinate reacts stereospecifically with bromine andnsubsequently couples with nucleophile to form the corresponding opticallynactive R1P(O)(OEt)X with retention of configuration at the phosphorus center.nFor α-amino-H-phosphinates, the transformation could be realized without the protection of the amino group.