Facile Synthesis\nof FimH Antagonist and Its Analogues:\nSimple Entry to Complex <i>C</i>‑Mannoside Inhibitors\nof <i>E. coli</i> Adhesion

Synthesizing FimH antagonists is challenging because\nof their densely\nfunctionalized and stereochemically complex <i>C</i>-mannoside\nstructures, resulting in low yields and lengthy processes. We present\nan efficient method for synthesizing <i>C</i>-mannoside\nFimH antagonists by nickel-catalyzed reductive coupling and stereocontrolled\nreduction, thereby significantly simplifying the process and enabling\nthe synthesis of FimH antagonists in just four steps with an overall\nyield of 34–50%. This efficient synthesis holds significant\npotential for the rapid development of analogues targeting the treatment\nof urinary tract infections or Crohn’s disease caused by <i>Escherichia coli</i> (<i>E. coli</i>).