| 氯沙坦的合成 |
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| 引用本文： | 闫起强,郭拥政,谢苏豪,祁伟,杨琰,王文峰.氯沙坦的合成[J].合成化学,2010,18(1). |
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| 作者姓名： | 闫起强 郭拥政 谢苏豪 祁伟 杨琰 王文峰 |
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| 作者单位： | 1. 北京赛科药业有限公司,研发部,北京,100021
2. 浙江新赛科药业有限公司,浙江,上虞,312369 |
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| 摘 要： | 以2-丁基-4-氯-5-羟甲基咪唑和5-(4-溴甲基联苯-2-基)-1-三苯甲基-1H-四唑为原料,通过氮烷基化、脱三苯甲烷保护基和还原反应合成了抗高血压药氯沙坦,总收率64%,其结构经1H NMR表征。
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| 关 键 词： | 氯沙坦 烷基化 脱保护 药物合成 |
Synthesis of Losartan |
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| YAN Qi-qiang,GUO Yong-zheng,XIE Su-hao,Qi Wei,YANG Yan,WANG Wen-feng.Synthesis of Losartan[J].Chinese Journal of Synthetic Chemistry,2010,18(1). |
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| Authors: | YAN Qi-qiang GUO Yong-zheng XIE Su-hao Qi Wei YANG Yan WANG Wen-feng |
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| Abstract: | Losartan in overall yield of 64% was synthesized from 2-butyl-4-chloro-5-hydroxymethyl-imidazole and 5-(4-bromomethyl-biphenyl -2-yl)-1-triphenylmethyl-1H-tetrazole by a three-step reaction of N-alkylation,deprotection(triphenylmethane protecting group) and reduction.The structure was characterized by ~1H NMR. |
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| Keywords: | Losartan N-alkylation deprotection drug synthesis |
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