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 invo...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.展开更多
基金the National Natural Science Foundation of China (No.20272012)the Special Research Grant for Doctoral Sites in Chinese Universities (No.20010730001).
文摘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.
