US2008214835A1PendingUtilityA1

Processes for preparing darifenacin hydrobromide

66
Assignee: TEVA PHARMACEUTICALS USA INC FPriority: Dec 27, 2005Filed: May 6, 2008Published: Sep 4, 2008
Est. expiryDec 27, 2025(expired)· nominal 20-yr term from priority
Inventors:Valeriano MerliAugusto CanavesiPaola Daverio
C07D 405/06C07D 207/09A61P 13/00C07D 207/48C07D 307/79
66
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Claims

Abstract

The invention encompasses processes for the preparation of darifenacin hydrobromide.

Claims

exact text as granted — not AI-modified
1 . N-protected-3-(S)-pyrrolidinol of the formula, 
       
         
           
           
               
               
           
         
       
       wherein X is S, SO 2 , Si, or CO, and R is phenyl, tolyl, ortho, meta, or para-xylyl, linear or branched C 1-10  alkyl, H, or CF 3 . 
     
     
         2 . The N-protected-3-(S)-pyrrolidinol of  claim 1 , wherein X is S and R is phenyl. 
     
     
         3 . The N-protected-3-(S)-pyrrolidinol of  claim 1 , wherein X is S and R is tolyl. 
     
     
         4 . The N-protected-3-(S)-pyrrolidinol of  claim 3 , having a melting temperature of about 108° C. to about 112° C. 
     
     
         5 . The N-protected-3-(S)-pyrrolidinol of  claim 1 , wherein X is S and R is xylyl. 
     
     
         6 . The N-protected-3-(S)-pyrrolidinol of  claim 1 , wherein X is S and R is linear or branched C 1-10  alkyl. 
     
     
         7 . The N-protected-3-(S)-pyrrolidinol of  claim 1 , wherein X is SO 2  and R is phenyl. 
     
     
         8 . The N-protected-3-(S)-pyrrolidinol of  claim 1 , wherein X is SO 2  and R is tolyl. 
     
     
         9 . The N-protected-3-(S)-pyrrolidinol of  claim 1 , wherein X is SO 2  and R is xylyl. 
     
     
         10 . The N-protected-3-(S)-pyrrolidinol of  claim 1 , wherein X is SO 2  and R is linear or branched C 1-10  alkyl. 
     
     
         11 . The N-protected-3-(S)-pyrrolidinol of  claim 1 , wherein X is Si and R is linear or branched C 1-10  alkyl. 
     
     
         12 . The N-protected-3-(S)-pyrrolidinol of  claim 1 , wherein X is CO and R is H. 
     
     
         13 . The N-protected-3-(S)-pyrrolidinol of  claim 1 , wherein X is CO and R is CF 3 . 
     
     
         14 . The N-protected-3-(S)-pyrrolidinol of  claim 1 , wherein X is CO and R is CH 3 .

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