Improvement Of The Synthesis Process Of Olmesartan Medoxomil

In order to improve the synthesis process of a new antihypertensive drug, olmesartan medoxomil was studied in this paper. Olmesartan medoxomil is a substituted imidazole compounds, mainly used in clinical treatment of hypertension ARB, which have a significant effect in terms of reducing the overall efficacy of diastolic blood pressure.After searching the existing technologies, a suitable process rout has been selected. Taking the ethyl 4-(1-hydroxy-1-methylethyl)-2-propyl-1H-imidazole-5-carboxylate(6) and 4-[2-(trityl tetrazolium-5-yl) phenyl] benzyl bromide(7) as the starting material, olmesartan medoxomil was synthesized by the four-step reaction which contained nucleophilic substitution reaction, hydrolysis reaction, esterification reaction and deprotection reaction.By adjusting the optimization of process parameters to produce the olmesartan medoxomil, the largest single impurity less than 0.1%. We obtained a low cost and simple process route, to perpare olmesartan medoxomil which meet the ICH standards.The structures of olmesartan medoxomil was identified by the data of IR、1H-NMR、13C-NMR、H-H COSY、DEPT、HSQC、HMBC、MS.