| 抗高血压药缬沙坦的新合成方法 |
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| 引用本文： | 邹江,杨琰,鲁峰,王文峰. 抗高血压药缬沙坦的新合成方法[J]. 化学试剂, 2009, 31(4) |
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| 作者姓名： | 邹江 杨琰 鲁峰 王文峰 |
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| 作者单位： | 北京赛科药业有限责任公司,北京,101111;北京赛科药业有限责任公司,北京,101111;北京赛科药业有限责任公司,北京,101111;北京赛科药业有限责任公司,北京,101111 |
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| 摘 要： | 以2N-三苯甲基-5-(4'-溴甲基联每2-基)四氮唑为原料,与L-缬氨酸甲酯盐酸盐反应制得N-[[2'-(2N-三苯甲基-四氮唑-5-基)-(1,1'-二苯基)-4-基]-甲基]-L-缬氨酸甲酯,然后经过脱三苯甲基保护、酰化、水解得到标题化合物,总收率49.8%.
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| 关 键 词： | 缬沙坦 血管紧张素Ⅱ受体拮抗剂 合成 |
New method for synthesis of antihypertensive drug valsartan |
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| ZOU Jiang,YANG Yan,LU Feng,WANG Wen-feng. New method for synthesis of antihypertensive drug valsartan[J]. Chemical Reagents, 2009, 31(4) |
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| Authors: | ZOU Jiang YANG Yan LU Feng WANG Wen-feng |
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| Affiliation: | Beijing Second Pharmaceutical Co.;Ltd.;Beijing 101111;China |
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| Abstract: | The reaction of 2N-trityl-5-(4'-methylbiphenyl-2-yl)tetrazole with L-valine methyl ester hydrochloride resulted in the formation of N-[[2'-(2N-trityl-tetrazol-5-yl)[1,1'-biphenyl]-4-yl] methyl]-L-valine methyl ester.Removal of the trityl protecting group produced N-[[2'-(1H-tetrazol-5-yl)-(1,1'-biphenyl)-4-yl]-methyl]-L-valine methyl ester.Acylation of N-[[2'-(1H-tetrazol-5-yl)-(1,1'-biphenyl)-4-yl]-methyl]-L-valine methyl ester with pentanoyl chloride resulted in the formation of N-(1-oxopentyl)-N-[[2'-(1H... |
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