Solid-phase parallel synthesis of azarene pyrrolidinones as factor Xa inhibitors

Abstract A focused library (4×14) prepared from 4-aminopyridine and 4-, 5-, and 6-azoindole templates was synthesized using 14 polymer supported 4-amido-2,3,5,6-tetrafluorophenyl (TFP) sulfonate esters inputs. Several compounds were identified as factor Xa inhibitors (IC 50 ≤0.1 μM) helping to establish the SAR among these four series of azarene pyrrolidinones.