Process for the synthesis of peptides containing a 4-hydroxy-proline substructure

Abstract

The present invention relates to processes for preparing peptides and to intermediates involved in such processes, e.g. a process for preparing a compound of formula VIII wherein R 12 and R 13 are as defined herein.

1 - 4 . (canceled) 
   
   
       5 . A compound of formula VI in free or salt form 
     
       
         
         
             
             
         
       
     
     wherein R 3 , R 4  and R 5  are each independently hydrogen or one or more substituents attached to each benzene ring, and are selected from hydroxy, amino, C 1-10 -alkyl, C 1-10 -alkoxy, C 1-10 -alkylamino, di-C 1-10 -alkylamino, carbamoyl, C 1-10 -alkylcarbamoyl, di-C 1-10 -alkylcarbamoyl, halo-C 1-10 -alkyl, halogeno or nitro, optionally protected by a removable protecting group;
 R 9  is —OH, —OM or —OMX, where M is metal and X is a nucleophilic substituent; and 
 R 10  is -M or -MX, where M is metal and X is a nucleophilic substituent. 
 
   
   
       6 - 10 . (canceled)