Abstract

Several phosphoramidate analogues of CMP- N-acetylneuraminic acid were prepared for evaluation as inhibitors of α-2,3- and α-2,6-sialyltransferase. Central to the synthesis was the oxidative coupling of an amino acid ester with an H-phosphonate to construct the phosphoramidate linkage. All compounds synthesized were weak inhibitors of both of the sialyltransferases as determined by an HPLC-based inhibition assay.

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