New processes for producing beta-alanine derivatives

Abstract

The present invention relates to processes for the preparation of β-alanine derivative shown by following formula (I): wherein R 1 is amino protective group, and R 2 is acyl group, or a salt thereof, which comprises, subjecting a compound of the formula (II): wherein R 1 is the same as defined above, and R 3 is protected carboxy, or a salt, to elimination reaction of carboxy protective group, and then to acylation reaction of amino group.

1 . A process for preparing a compound of the formula (I):  
       
         
           
           
               
               
           
         
       
       wherein R 1  is amino protective group, and 
 R 2  is acyl group, or a salt thereof, which comprises, subjecting a compound of the formula (II):  
                     
 wherein R 1  is the same as defined above, and  
 R 3  is protected carboxy, or a salt thereof, to elimination reaction of carboxy protective group, and then to acylation reaction of amino group.  
 
     
     
         2 . A process for preparing a compound of the formula (III):  
       
         
           
           
               
               
           
         
       
       wherein R 2  is acyl group, or a salt thereof, subjecting a compound of the formula (I) obtained by the process of  claim 1 , to elimination reaction of amino protective group.  
     
     
         3 . A process of  claim 1  or  2 , wherein R 1  is lower alkoxycarbonyl, 
 R 2  is lower alkanoyl, and  
 R 3  is lower alkoxycarbonyl.  
 
     
     
         4 . A process of  claim 3 , wherein R 1  is tert-butoxycarbonyl, 
 R 2  is acetyl, and    is R 3  is methoxycarbonyl.    
     
     
         5 . A compound, which is produced by the process of  claim 1 ,  2 ,  3  or  4 .  
     
     
         6 . N-[(R)-1-[3-(4-piperidyl)propionyl]-3-piperidyl-carbonyl]-2(S)-acetylamino-β-alanine trihydrate.