A NOVEL PROCESS FOR THE PREPARATION OF VALSARTAN

摘要

PURPOSE: A method for preparing valsartan which is an antiotensin receptor blocker is provided to synthesize valsartan without by-product in high yield and high purity. CONSTITUTION: A method for preparing N-(1-oxopentyl)-N-(2'-(1H-tetrazole-5-yl)[1,1'-biphenyl-4-yl]methyl-L-valine(valsartan) comprises: a step of reacting 2'-cyanobiphenyl-4-methylbromide of structural formula 2 with (L)-valiine ester derivative of structural formula 3 in halogen alkane solvent without a base to obtain N-[(2'-cyanobiphenyl-4-yl)methyl]-(L)-valine ester derivative of structural formula 4; a step of reaction the compound of structural formula 4 with valeryl chloride in an aromatic organic solvent to obtain N-valeryl-N-[(2'-cyanobiphenyl-4-yl)methyl]-(L)-valine ester derivative of structural formula 6; and a step of reacting the compound of structural formula 6 with alkali metal azide and zinc halide in a pyridine solvent.