Efficient Synthesis of Anticoagulant Fondaparinux via Orthogonal One‐Pot Glycosylation and Microwave‐Assisted Simultaneous O,N‐Sulfonation

Comprehensive Summary Here, we report an effective approach to the synthesis of anticoagulant fondaparinux, utilizing orthogonal one‐pot [1+2+2] glycosylation, simultaneous O , N ‐sulfation and global debenzylation at atmospheric pressure as key steps. The synthetic route was achieved through the longest linear sequence of 12 steps with 19% overall yield from a commercially available disaccharide. The present synthetic route remarkably enhances synthetic efficiency and streamlines the purification process, thereby opening up a new avenue for the large‐scale synthesis of fondaparinux and relevant heparin fragments.