Efficient process for the preparation of a factor Xa inhibitor

Abstract

The present invention relates to the process for the preparation of the compound of Formula I: from its corresponding 3-cyano-4-fluorophenyl-pyrazole and intermediates useful therein.

1 - 16 . (canceled)  
     
     
         17 . A process according to claim  1 , wherein the compound of Formula IVa is prepared by the process, comprising:  
       
         
           
           
               
               
           
         
         (b) coupling compounds of Formulas II and III to form a compound of Formula IVa.  
       
     
     
         18 . A process according to  claim 17 , wherein the compound of Formula IVa is used without purification in (c).  
     
     
         19 . A process according to  claim 17 , wherein (b) is performed by contacting a compound of Formula II with an acid activator, in a solvent and a first base, followed by contacting the resulting solution with a compound of Formula III.  
     
     
         20 . A process according to  claim 19 , wherein (b) is performed by contacting a compound of Formula II with oxalyl chloride in acetonitrile and pyridine, followed by contacting the resulting solution with a compound of Formula III.  
     
     
         21 . A process according to  claim 20 , wherein after a compound of Formula II has been contacted with a compound of Formula III, a second base is added to the reaction solution.  
     
     
         22 . A process according to  claim 21 , wherein the second base is diisopropylethylamine.  
     
     
         23 - 27 . (canceled)  
     
     
         29 . A compound of Formula Va:  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt form thereof.  
     
     
         30 - 31 . (canceled)