Yang Li
2006
Citations
0
Influential Citations
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Journal
Chinese Journal of New Drugs
Abstract
Objective:To simplify a synthetic procedure of losartan.Methods:An intermediate 2-butyl-4(5)-chloroimidazole-5(4)-carboxaldehyde(4) was prepared from pentanitrile via a three-step process.Additional intermediate N-(triphenylmethyl)-5-[4′-(bromomethyl)biphenyl-2-yl] tetrazole (8) was obtained from 2-cyano-4′-methyl-biphenyl via a three-step process.The target product losartan was synthesized by the combination of compound 4 to compound 8 via steps including N-alkylation,re- duction and detritylation.Results:Chemical structures of intermediate and target products were verified by IR,~1HNMR,MS and EI.The total yield of the target product was 51.8% (calculating from pentani- trile).Conclusion:This synthetic procedure with accessible starting materials and easily manipulation is worthy for the further pilot manufacture.