Elagolix Sodium Compositions and Processes

Abstract

The present invention relates to compositions of elagolix sodium, and process and intermediates for the preparation thereof.

We claim: 
     
         1 . A salt of 3-[(2R)-2-amino-2-phenylethyl]-5-(2-fluoro-3-methoxyphenyl)-1-{[2-fluoro-6-(trifluoromethyl)phenyl]methyl}-6-methylpyrimidine-2,4(1H,3H)-dione (Compound IIa): 
       
         
           
           
               
               
           
         
       
     
     
         2 . A process for preparing elagolix sodium (Compound (I)) in substantially pure form comprising, using, as an intermediate in the process, the salt of  claim 1 . 
     
     
         3 . The process of  claim 2 , further comprising, isolating the salt of Compound (IIa) to provide an isolated salt of Compound (IIa). 
     
     
         4 . The process of  claim 3 , wherein the isolated salt of Compound (IIa) is in crystalline form. 
     
     
         5 . A composition prepared by the process of  claim 2 , the composition comprising Compound (I) and Compound (IIa). 
     
     
         6 . The composition of  claim 5 , wherein the composition comprises not more than 0.70 weight percent of Compound (IIa). 
     
     
         7 . The composition of  claim 6 , wherein the Compound (IIa) is in crystalline form. 
     
     
         8 . The composition of  claim 7 , wherein the crystalline form of Compound (IIa) has an X-ray powder diffraction pattern comprising peaks at ±0.2 of 8.0, 11.5, 12.0, 12.5, 13.5, 15.4, 16.8, 17.3, 18.7, and 20.0° 2θ, when measured at about 25° C. with Cu-Kα1 radiation at 1.5406 {acute over (Å)}.