Practical synthesis and regioselective alkylation of methyl 4 (5)-(pentafluoroethyl)-2-propylimidazole-5 (4)-carboxylate to give DuP 532, a potent angiotensin II …

ME Pierce, DJ Carini, GF Huhn, GJ Wells…

Index: Pierce, Michael E.; Carini, David J.; Huhn, George F.; Wells, Gregory J.; Arnett, John F. Journal of Organic Chemistry, 1993 , vol. 58, # 17 p. 4642 - 4645

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Citation Number: 33

Abstract

DuP 753 (1, losartan) is a nonpeptide angiotensin I1 antagonist which is in phase I11 clinical trials as an orally active antihypertensive agent. lJ Ita major active metabolite, the imidazole-5-carboxylic acid, is not orally a~ tive.~ DuP 532 (2) is under development as an analogue that does not require metabolic activation and has been found to be longer acting and about three times more potent than DuP 753 when given orally to renal hypertensive ...