AN IMPROVED PROCESS FOR THE PREPARATION OF VALSARTAN

摘要

PURPOSE: A method for preparation of valsartan used in therapeutic agent of hypertension or heart failure is provided to ensure economic and reaction process for massive production. CONSTITUTION: A method for preparing N-(1-oxopentyl)-N-[(2'-(1H-tetrazole-5-yl)[1,1'-bipenyl]-4-yl]methyl]-L-valine(valsartan) of structural formula 1 comprises: a step of reacting 2'-cyanobipenyl-4-carboxyaldehyde of structural formula 2 with (L)-valine derivative under the presence of base in low alcohol of 1-4 carbon atoms to produce N-[(2'-cyanobipenyl-4-yl)methyl]-(L)-valine of structural formula 4; a step of reacting the compound of structural formula 4 with valeryl chloride in organic solvent to produce N-valeryl-N-[(2'-cyanobiphenyl-4-yl)methyl]-(L)-valine of structural formula 6; and a step of reacting the compound of structural formula 6 with alkali metal azide and halogenized zinc in aromatic hetero cyclic compound solvent.