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 - 34 . (canceled) 
     
     
         35 . A compound of formula (III): 
       
         
           
           
               
               
           
         
         wherein R 1  is C 1 -C 4  alkyl; X is halogen or triflate; and PG 4  is hydrogen or a hydroxy protecting group. 
       
     
     
         36 . The compound of  claim 35 , wherein X is iodine. 
     
     
         37 . The compound of  claim 35 , wherein R 1  is methyl. 
     
     
         38 . The compound of  claim 35 , wherein PG 4  is hydrogen. 
     
     
         39 . The compound of  claim 35  represented by the following structures: 
       
         
           
           
               
               
           
         
         wherein PG 4  is hydrogen or a hydroxy protecting group. 
       
     
     
         40 - 46 . (canceled) 
     
     
         48 . The compound of  claim 39 , wherein PG 4  is a hydroxy protecting group. 
     
     
         49 . A process of using a compound of  claim 35  to make a compound of formula (I); 
       
         
           
           
               
               
           
         
         wherein R 1  is C 1 -C 4  alkyl. 
       
     
     
         50 . A process of using a compound of  claim 35  to make a compound of formula (G); 
       
         
           
           
               
               
           
         
         wherein R 1  is C 1 -C 4  alkyl and PG 1  is an amine protecting group.