Processes for intermediates for macrocyclic compounds

Abstract

The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates: wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , n 1 , m, p Z 1 , Z 2 , and Z 3 are as describe in the specification. The invention also relates to compounds of formula (I) which are antagonists of the motilin receptor and are useful in the treatment of disorders associated with this receptor and with or with motility dysfunction.

1 - 29 . (canceled) 
     
     
         30 . A compound of formula (II): 
       
         
           
           
               
               
           
         
         wherein R 1  is C 1 -C 4  alkyl; X is halogen or triflate; and PG 3  is hydrogen or an ester protecting group. 
       
     
     
         31 . The compound of  claim 30 , wherein X is iodine. 
     
     
         32 . The compound of  claim 30 , wherein R 1  is methyl. 
     
     
         33 . The compound of  claim 30 , wherein PG 3  is an alkyl group or an alkyl group substituted with an aryl group. 
     
     
         34 . The compound of  claim 30  represented by the following structures: 
       
         
           
           
               
               
           
         
         wherein PG 3  is hydrogen or an ester protecting group. 
       
     
     
         35 - 46 . (canceled) 
     
     
         47 . The compound of  claim 34 , wherein PG 3  is hydrogen. 
     
     
         48 . The compound of  claim 34 , wherein PG 3  is an alkyl group or an alkyl group substituted with an aryl group. 
     
     
         49 . The compound of  claim 48 , wherein PG 3  is methyl. 
     
     
         50 . The compound of  claim 48 , wherein PG 3  is ethyl. 
     
     
         51 . The compound of  claim 48 , wherein PG 3  is benzyl. 
     
     
         52 . A process of using a compound of  claim 30  to make a compound of formula (I); 
       
         
           
           
               
               
           
         
       
       wherein R 1  is C 1 -C 4  alkyl. 
     
     
         53 . A process of using a compound of  claim 30  to make a compound of formula (G); 
       
         
           
           
               
               
           
         
         wherein R 1  is C 1 -C 4  alkyl and PG 1  is an amine protecting group.