缬沙坦的合成

Synthesis of Valsartan

以N-(三苯基甲基)-5-(4'-溴甲基联苯-2-基)四氮唑为原料,与N-戊酰基-L-缬氨酸甲酯反应制得3-甲基-2-[戊酰基-[[4-[2-(1-三苯甲基四唑-5-基)苯基]苯基]甲基]氨基]丁酸甲酯,然后经过脱三苯基保护、水解反应得到缬沙坦,总收率52%。该工艺具有路线短、收率高、成本低等优点,适于工业化生产。

The reaction of N-（triphenylmethyl）-5-（4＇-bromomethylbiphenyl-2-yl-）tetrazole with methyl N-pentanoyl-L-valinate resulted in the formation of methyl N-pentanoyl-N-{[2＇-（1-trityl-1H-tetrazol-5-yl）biphenyl-4-yl]methyl}-L-valinate.Deprotection of triphenylmethyl group and hydrolysis of the methyl ester could be carried out to achieve the anticipated product,valsartan.The total yield of which was 52 %.This method overcomes many of the drawbacks associated with the previously reported syntheses and is more suitable for industrial production.