Process of Preparation of Olanzapine Form I

Abstract

A process for the preparation of polymorph Form I of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2.3-b][1,5]benzodiazepine, or olanzapine.

1 - 17 . (canceled) 
     
     
         18 . Olanzapine Form I having a polymorphic purity of at least 98%, having an X-ray diffraction pattern characterized by the following interplanar spacing values (d) and relative intensities (I/I 0 ) 
       
         
           
                 
                 
                 
               
                     
                     
                 
                     
                   d value 
                   I/I o  value 
                 
                     
                     
                 
                     
                 
                 
                 
                 
               
                     
                   9.9463 
                   100.0 
                 
                     
                   8.5579 
                   15.18 
                 
                     
                   6.8862 
                   14.73 
                 
                     
                   4.8333 
                   68.37 
                 
                     
                   4.7255 
                   21.88 
                 
                     
                   4.533 
                   17.83 
                 
                     
                   4.2346 
                   18.88 
                 
                     
                   4.855 
                   17.29 
                 
                     
                   3.7489 
                   10.64 
                 
                     
                   3.6983 
                   14.65. 
                 
                     
                     
                 
             
                
                
                
               
               
                
               
            
             
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         19 . Olanzapine Form I of  claim 18  having a polymorphic purity of at least 99%. 
     
     
         20 . Olanzapine Form I of  claim 18  substantially free of olanzapine Form II. 
     
     
         21 . A pharmaceutical composition comprising a compound of  claim 18  and a pharmaceutically acceptable diluent or carrier therefor. 
     
     
         22 . A method of treating a person suffering from or being, susceptible to psychosis, acute mania, or mild anxiety states which comprises administering to said person an effective amount of a compound of  claim 18 .