One-pot facile synthesis of 4-amino-1,8-naphthalimide derived Tröger's bases via a nucleophilic displacement approach
One-pot facile synthesis of 4-amino-1,8-naphthalimide derived Tröger's bases via a nucleophilic displacement approach
  We report here a novel one-pot synthetic strategy for the synthesis of a family of N-alkyl-1,8-naphthalimide based Tröger's bases via a nucleophilic substitution reaction of a common ‘precursor’ (or a ‘synthon’) N-aryl-1,8-naphthalimide Tröger's base heated at 80 °C in neat aliphatic primary amine, in overall yield of 65–96%. This methodology provides an efficient and one-step facile route to design 1,8-naphthalimide derived Tröger's base structures in analytically pure form without the use of column chromatography purification, that can be used in medicinal chemistry and as supramolecular scaffolds. We also report the formation of the corresponding anhydride, and the crystallographic analysis of two of the resulting products, that of the N-phenyl-4-amino-1,8-naphthalimide and the anhydride derived Tröger's bases.
  
  
  7321-7329
  
    
      Shanmugaraju, Sankarasekaran
      
        193c398c-9ba6-4bc4-8204-ae483b9f9fda
      
     
  
    
      Mcadams, Deirdre
      
        d658aa00-5db6-403d-9735-e448f56eb07d
      
     
  
    
      Pancotti, Francesca
      
        acd90cde-0c00-4f78-a1d8-36fe5f0c4833
      
     
  
    
      Hawes, Chris S.
      
        c3d2ccc1-40e2-4bf7-9eef-b4bfe8b8af20
      
     
  
    
      Veale, Emma B.
      
        92576e03-2cf9-48fc-80f2-9907e7331390
      
     
  
    
      Kitchen, Jonathan A.
      
        3999f5cb-d53e-4c51-b750-627bd2a1b9b6
      
     
  
    
      Gunnlaugsson, Thorfinnur
      
        bbfcaaa6-2aca-47c9-9b7b-954442218f50
      
     
  
  
   
  
  
    
    
  
    
    
  
    
      21 September 2017
    
    
  
  
    
      Shanmugaraju, Sankarasekaran
      
        193c398c-9ba6-4bc4-8204-ae483b9f9fda
      
     
  
    
      Mcadams, Deirdre
      
        d658aa00-5db6-403d-9735-e448f56eb07d
      
     
  
    
      Pancotti, Francesca
      
        acd90cde-0c00-4f78-a1d8-36fe5f0c4833
      
     
  
    
      Hawes, Chris S.
      
        c3d2ccc1-40e2-4bf7-9eef-b4bfe8b8af20
      
     
  
    
      Veale, Emma B.
      
        92576e03-2cf9-48fc-80f2-9907e7331390
      
     
  
    
      Kitchen, Jonathan A.
      
        3999f5cb-d53e-4c51-b750-627bd2a1b9b6
      
     
  
    
      Gunnlaugsson, Thorfinnur
      
        bbfcaaa6-2aca-47c9-9b7b-954442218f50
      
     
  
       
    
 
  
    
      
  
  
  
  
  
  
    Shanmugaraju, Sankarasekaran, Mcadams, Deirdre, Pancotti, Francesca, Hawes, Chris S., Veale, Emma B., Kitchen, Jonathan A. and Gunnlaugsson, Thorfinnur
  
  
  
  
   
    (2017)
  
  
    
    One-pot facile synthesis of 4-amino-1,8-naphthalimide derived Tröger's bases via a nucleophilic displacement approach.
  
  
  
  
    Organic & Biomolecular Chemistry, 15 (35), .
  
   (doi:10.1039/C7OB01835E). 
  
  
   
  
  
  
  
  
   
  
    
    
      
        
          Abstract
          We report here a novel one-pot synthetic strategy for the synthesis of a family of N-alkyl-1,8-naphthalimide based Tröger's bases via a nucleophilic substitution reaction of a common ‘precursor’ (or a ‘synthon’) N-aryl-1,8-naphthalimide Tröger's base heated at 80 °C in neat aliphatic primary amine, in overall yield of 65–96%. This methodology provides an efficient and one-step facile route to design 1,8-naphthalimide derived Tröger's base structures in analytically pure form without the use of column chromatography purification, that can be used in medicinal chemistry and as supramolecular scaffolds. We also report the formation of the corresponding anhydride, and the crystallographic analysis of two of the resulting products, that of the N-phenyl-4-amino-1,8-naphthalimide and the anhydride derived Tröger's bases.
         
      
      
        
          
            
  
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      Accepted/In Press date: 14 August 2017
 
    
      e-pub ahead of print date: 14 August 2017
 
    
      Published date: 21 September 2017
 
    
  
  
    
  
    
  
    
  
    
  
    
  
    
  
    
  
    
  
  
        Identifiers
        Local EPrints ID: 414810
        URI: http://eprints.soton.ac.uk/id/eprint/414810
        
          
        
        
        
          ISSN: 1477-0520
        
        
          PURE UUID: 0586c0ce-6066-4374-a937-7e1a1c3258c2
        
  
    
        
          
        
    
        
          
        
    
        
          
        
    
        
          
        
    
        
          
        
    
        
          
            
              
            
          
        
    
        
          
        
    
  
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  Date deposited: 11 Oct 2017 16:31
  Last modified: 16 Mar 2024 05:48
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      Contributors
      
          
          Author:
          
            
            
              Sankarasekaran Shanmugaraju
            
          
        
      
          
          Author:
          
            
            
              Deirdre Mcadams
            
          
        
      
          
          Author:
          
            
            
              Francesca Pancotti
            
          
        
      
          
          Author:
          
            
            
              Chris S. Hawes
            
          
        
      
          
          Author:
          
            
            
              Emma B. Veale
            
          
        
      
          
          Author:
          
            
              
              
                Jonathan A. Kitchen
              
              
                
              
            
            
          
         
      
          
          Author:
          
            
            
              Thorfinnur Gunnlaugsson
            
          
        
      
      
      
    
  
   
  
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