Synthesis Process Of Fimasartan

Fimasartan was developed by Boryung Pharmaceutical. It was an angiotensin? receptor antagonist(ARB) antihypertensive drugs which was used for the treatment of hypertension. This article was completed on the basis of literature about the fimasartan chemical synthesis. After analyzing the different route we choose a suitable synthetic route and propose a new synthesis process.We used valeronitrile as starting materials and synthetic pentamidine hydro chloride, pentamidine hydrochloride react with acetyl diethyl succinate, then syn thesis of 2-(2-n-butyl-4-hydroxy-6-methyl-pyrimidin-5-yl)-N, N-dimethylacetamide.In this step we used EDCI as carbonyl activating reagents, triethylamine as ac id binding agent. The reaction yield was 86% that higher than the yield report ed in the literature(80%).2-(2-n-butyl-4-hydroxy-6-methyl-pyrimidin-5-yl)-N, N-d imethylacetamide occur N-alkylation reaction under the catalysis of LIH, then s ynthesis fimasartan. This step examines a variety of factors which effect the yi eld of ths step and achieve an optimal reaction conditions. The reaction time was 76 h.Referenced related literature about Fimasartan, crystallization effect of the non-horse-sand potassium in different solvents was investigated. Then confirmed by TG-DSC and XRD.