Abstract The first diastereoselective total synthesis of 5-substituted morpholine-3- phosphonic acids is reported. The principal feature of the synthesis is the introduction of a dimethyl phosphonate group into 5-substituted morpholin-3-ones. The procedure is based on the preparation of N-Boc-(S)-5-phenyl-and N-Boc-(S)-5-benzylmorpholin-3-one from l- phenylglycine and l-phenylalanine methyl esters, followed by the formation of the 3- ...
