A Fast and Effective Hydrogenation Process of Protected
Pentasaccharide: A Key Step in the Synthesis of Fondaparinux Sodium
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Abstract
An
improved method for the simultaneous removal of <i>O</i>-benzyl and <i>N</i>-carboxybenzyl groups as well as reducing
azide groups to amines in protected heparin-like pentasaccharides,
a key process in fondaparinux sodium synthesis, is reported. Under
catalytic transfer hydrogenation conditions, using readily available
and inexpensive ammonium formate, the hydrogenolysis is done in less
than an hour in good yield and purity. This procedure represents a
major advantage over the previously published procedures, the latter
of which involve several hours/days of hydrogenation reaction under
catalytic reduction using gaseous hydrogen