| 缬沙坦的合成 |
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| 引用本文： | 任洪发.缬沙坦的合成[J].广东化工,2011,38(6):88+80-88,80. |
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| 作者姓名： | 任洪发 |
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| 作者单位： | 广东肇庆星湖生物科技股份有限公司,广东,肇庆,526070 |
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| 摘 要： | 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。
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| 关 键 词： | 缬沙坦 N-戊酰基-L-缬氨酸甲酯 合成 |
Synthesis of Valsartan |
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| Ren Hongfa.Synthesis of Valsartan[J].Guangdong Chemical Industry,2011,38(6):88+80-88,80. |
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| Authors: | Ren Hongfa |
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| Affiliation: | Ren Hongfa(Star Lake Bioscience Co.Inc.Zhaoqing Guangdong,Zhaoqing 526070,China) |
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| Abstract: | 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 suita... |
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| Keywords: | valsartan methyl N-pentanoyl-L-valinate synthesis |
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