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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.
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