Improvement of Process for Olmesartan Medoxomil

OBJECTIVE To improve the synthesis process for olmesartan medoxomil. METHODS Olemsartan medoxomil( 1 ) was synthesized using 2-cyano-4'-methylbiphenyl( 2 ) as the starting material, via bromination, “one-pot” tandem N-alkylation/saponification-esterification sequence and tetrazolium reaction. RESULTS The total yield was 46.5% basing on the starting material 2-cyano-4'-methylbiphenyl over 3 steps. CONCLUSION The improved process is practical and suitable for industrial scaling-up.