Acetone solvate crystals of trityl omesartan medoxomil

Abstract

Acetone solvate crystals of trityl olmesartan medoxomil are provided.

1 . Acetone solvate crystals of trityl olmesartan medoxomil which exhibit peaks at diffraction angle 2θ of the following, in powder X-ray crystal diffraction: 10.2, 15.7, 19.3, 20.7, and 24.1 degree with error margin of ±0.2 degree. 
     
     
         2 . Acetone solvate crystals of trityl olmesartan medoxomil which exhibit a peak at 96.3° C. in differential scanning calorimeter analysis of the crystals. 
     
     
         3 . The acetone solvate crystals of  claim 1 , which comprise 1 mol of acetone per 1 mol of trityl olmesartan medoxomil. 
     
     
         4 . The acetone solvate crystals of  claim 2 , which comprise 1 mol of acetone per 1 mol of trityl olmesartan medoxomil. 
     
     
         5 . A method for producing the acentone solvate crystals according to  claim 1 , which comprises the following steps:
 (step 1) a step of tritylation and DMDO esterification of olmesartan in an acetone solvent optionally containing water;   (step 2) a step of precipitating acetone solvate crystals of trityl olmesartan medoxomil from the reaction mixture obtained in (step 1); and   (step 3) a step of isolating the acetone solvate crystals obtained in (step 2) and drying the acetone solvate crystals in vacuo at 60° C.   
     
     
         6 . A method for producing the acetone solvate crystals according to  claim 1 , which comprises the following steps:
 (step 1) reacting olmesartan with trityl halide and with DMDO halide in an acetone solvent in the presence of a base; and   (step 2) precipitating the acetone solvate crystals of trityl olmesartan medoxomil from the reaction mixture obtained in (step 1),   
       wherein the trityl halide in (step 1) is trityl chloride or trityl bromide, and wherein the DMDO halide in (step 1) is DMDO chloride or DMDO bromide, and wherein the base in (step 1) is triethylamine, diisopropylethylamine, pyridine, or 1,8-diazabicyclo[5,4,0]-7-undecene (DBU). 
     
     
         7 . The method according to  claim 6 , wherein the trityl halide in (step 1) is trityl chloride, and wherein the DMDO halide in (step 1) is DMDO chloride, and wherein the base in (step 1) is 1,8-diazabicyclo[5,4,0]-7-undecene (DBU). 
     
     
         8 . A method for producing olmesartan medoxomil, which comprises a step of removing the trityl group from the acetone solvate crystals of trityl olmesartan medoxomil according to  claim 1 . 
     
     
         9 . A method for producing olmesartan medoxomil, which comprises a step of removing the trityl group from the acetone solvate crystals of trityl olmesartan medoxomil according to  claim 2 . 
     
     
         10 . A method for producing olmesartan medoxomil, which comprises a step of removing the trityl group from the acetone solvate crystals of trityl olmesartan medoxomil obtained by the method according to  claim 5 . 
     
     
         11 . A method for producing olmesartan medoxomil, which comprises a step of removing the trityl group from the acetone solvate crystals of trityl olmesartan medoxomil obtained by the method according to  claim 6 . 
     
     
         12 . A method for producing olmesartan medoxomil, which comprises a step of removing the trityl group from the acetone solvate crystals of trityl olmesartan medoxomil obtained by the method according to  claim 7 .