Study On The Synthesis Of Valsartan From Antihypertensive Drugs

With the development of china economy, hypertension has been commonly encountered disease and one of the most dangerous killers of Chinese group. As a novel angiotensin Ⅱ inhibitor, valsartan which was developed by Novartis has been widely used to treat high blood pressure in the world. In today china, the market scale of valsartan keeps enlarging for its excellent curative effect on hypertension.In this thesis, a practical and economical synthetic route of the anti-hypertensive medicine valsartan was developed after experiment verification and reasonable screening of literature methods. With cheap L-Valine as the starting material, followed by esterification with methanol, alkylation with4’-Bromoethyl-2-cyanobiphenyl, acylation with valeryl chloride, cyclation with tributyltin azide, hydrolysis procedure to give valsartan. The total yield is50.2%, and the purity of final product is99%. The specific rotation value is-63°.The process had following advantages:(1) Short route (5steps) and high yield.(2) Intermediates did not require purification by column chromatography. Less adjuvant material assisted.(3) Simple operation and low cost.