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Valsartan 1,one of the most important agents used in antihypertensive therapy today,was synthesized starting from L-valin methyl ester hydrochloride 2 through four steps in an overall yield of 60%.The key step involves the palladium-catalyzed Suzuki coupling.This method overcomes many of the drawbacks associated with the previously reported syntheses and is more suitable for industrial production.
Valsartan 1, one of the most important agents used in antihypertensive therapy today, was formed starting from L-valin methyl ester hydrochloride 2 through four steps in an overall yield of 60%. The key step involves the palladium-catalyzed Suzuki coupling. This method overcomes many of the drawbacks associated with the previously reported syntheses and is more suitable for industrial production.