Synthesis of Anticoagulant Pentasaccharide Fondaparinux via 3,5-Dimethyl-4-(2'-phenylethynylphenyl)phenyl Glycosides.

Here, we disclosed a convenient procedure for the preparation of EPP [3,5-dimethyl-4-(2'-phenylethynylphenyl)phenyl] glycosides and their application to an effective synthesis of fondaparinux, the clinically approved anticoagulant heparin pentasaccharide. The use of EPP glycosides in the one-pot orthogonal glycosylation for the synthesis of heparin-like tetrasaccharides has also been achieved.