Process for producing 4-aminoquinazoline compound

Abstract

A 4-aminoquinazoline derivative can be obtained by the steps of reacting quinazolin-4-one or its derivative with a chlorinating agent in a first organic solvent in the presence of an organic base, and subsequently reacting the reaction product with an amine compound represented by the formula R 5 —NH—R 6 (each of R 5 and R 6 represents hydrogen or an optionally substituted hydrocarbyl group) in the presence of a second organic solvent.

1 . A process for preparing a 4-aminoquinazoline compound having the formula (3): 
       
         
           
           
               
               
           
         
         in which each of R 1 , R 2 , R 3  and R 4  independently represents a group not participating the below-mentioned reaction, or R 1 , R 2 , R 3  and R 4  are combined to form a ring, and each of R 5  and R 6  independently represents a hydrogen atom or a hydrocarbyl group which can have a 
         which comprises: 
         a first step of reacting a quinazolin-4-one compound having the formula (1): 
       
       
         
           
           
               
               
           
         
         in which R 1 , R 2 , R 3  and R 4  have the same meaning as above, 
         with a chlorinating agent in a first organic solvent in the presence of an organic base and 
         a second step for reacting a reaction product of the first step with an amine compound having the formula (2):
   R 5 —NH—R 6   (2) 
 
         in which R 5  and R 6  have the same meaning as above, 
         in the presence of a second organic solvent.