New and improved manufacturing process for valsartan

…, BK Sinha, K Mukkanti, R Dandala

Index: Kumar N, Senthil; Reddy, Shankar B.; Sinha, Brajesh Kumar; Mukkanti, Kagga; Dandala, Ramesh Organic Process Research and Development, 2009 , vol. 13, # 6 p. 1185 - 1189

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Citation Number: 12

Abstract

Problems associated with this synthetic process have been (a) the use of highly toxic tri-n-butyltinazide in the conversion of compound 5 to compound 6(8, 9) at the penultimate stage of valsartan synthesis, (b) contamination of final product with traces of toxic tin metal, (c) racemisation of valsartan up to 15% during hydrolysis under basic conditions,(10) and (d) low purity and low yield of valsartan. To achieve acceptable purity, chiral purity and acceptable limit of tin as per ICH ...