Valsartan Improved Synthesis And Industrialization

The synthesis of Valsartan starting from L-Valine methyl ester and 2'-Cyano-4-Bromomethyl-biphenyl was studied. The results show that the optical purity of the product is over 99%, The content of impurities is less than 1%, and the total yield reaches 30%. The synthetic process of 2'-Cyano-4-Bromomethyl-biphenyl as well as other intermediates was also optimized. The structure of the product was characterized. The process was industrialized according to GMP rules and remarkable economic benefit has been gained.