Process for preparing alpha-carboxamide pyrrolidine derivatives

Abstract

The disclosure relates to novel processes for preparing α-carboxamide pyrrolidine derivatives, in particular (2S, 5R)-5-(4-((2-fluorobenzyl)oxy)phenyl)pyrrolidine-2-carboxamide, and to novel intermediates for use in said process along with processes for preparing said intermediates.

1 - 8 . (canceled) 
     
     
         9 . A compound of formula (I): 
       
         
           
           
               
               
           
         
         wherein P 1  represents a protecting group selected from: 9-fluorenylmethyloxycarbonyl (FMOC); acetyl (Ac); benzoyl (Bz); a carbamate; p-methoxyphenyl (PMP); tosyl (Ts); a sulfonamide selected from Nosyl and Nps and trifluoroacetyl. 
       
     
     
         10 - 49 . (canceled) 
     
     
         50 . The compound of  claim 9 , wherein P 1  is 9-fluorenylmethyloxycarbonyl (FMOC). 
     
     
         51 . The compound of  claim 9 , wherein P 1  is acetyl (Ac). 
     
     
         52 . The compound of  claim 9 , wherein P 1  is benzoyl (Bz). 
     
     
         53 . The compound of  claim 9 , wherein P 1  is a carbamate. 
     
     
         54 . The compound of  claim 9 , wherein P 1  is p-methoxyphenyl (PMP). 
     
     
         55 . The compound of  claim 9 , wherein P 1  is tosyl (Ts). 
     
     
         56 . The compound of  claim 9 , wherein P 1  is Nosyl. 
     
     
         57 . The compound of  claim 9 , wherein P 1  is Nps. 
     
     
         58 . The compound of  claim 9 , wherein P 1  is trifluoroacetyl.