Synthesis of Valsartan as drug for the treatment of hypertension

Abstract

The synthesis of valsartan (1), one of the most currently used pharmaceutical agent in antihypertensive therapy, was described through five steps in an overall yield of 54 % starting from 4’-methyl-2-cyanobiphenyl (2). The key step involved tetrazole ring formation catalyzed by Lewis acid. The structures of synthesized compounds were confirmed by means of NMR and MS spectroscopíe.