A. Grandas et al., PHOSPHITYLATION OF PRIMARY CARBOXAMIDES - SYNTHESIS OF PEPTIDE-OLIGONUCLEOTIDE CONJUGATES WITH ACYLPHOSPHORAMIDATE LINKAGES, Nucleosides & nucleotides, 14(3-5), 1995, pp. 825-828
N-acylphosphoramidates can be obtained from the reaction of phosphityl
ated primary carboxamides and an alcohol in the presence of an acid ca
talyst such as tetrazole and subsequent oxidation. The reaction is use
ful for the preparation of peptide-oligonucleotide conjugates.