A high-throughput process for valsartan

U Beutler, M Boehm, PC Fuenfschilling…

Index: Beutler, Ulrich; Boehm, Matthias; Fuenfschilling, Peter C.; Heinz, Thomas; Mutz, Jean-Paul; Onken, Ulrich; Mueller, Martin; Zaugg, Werner Organic Process Research and Development, 2007 , vol. 11, # 5 p. 892 - 898

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Citation Number: 16

Abstract

With the redesign of three chemical steps, the throughput of the valsartan manufacturing process could be significantly increased, and with the substitution of chlorobenzene with cyclohexane in the bromination of 4′-methyl-biphenyl-2-carbonitrile (6) to 4′-bromomethyl- biphenyl-2-carbonitrile (5), halogenated solvents are no longer used in the whole valsartan production process. The alkylation of (S)-2-amino-3-methyl-butyric acid benzyl ester (8) ...