| 一种非索非那定关键中间体的合成研究 |
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| 引用本文： | 卢小逸,吴文良,董道敏,张启明.一种非索非那定关键中间体的合成研究[J].浙江化工,2012,43(6):25-26. |
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| 作者姓名： | 卢小逸 吴文良 董道敏 张启明 |
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| 作者单位： | 浙江启明药业有限公司,浙江上虞,312369 |
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| 摘 要： | 以4-（4-氯丁酰基）-α,α-二甲基苯乙酸甲酯（5）为原料，与4-氰基哌啶（4）缩合，再与二苯甲酮（2）反应得到了2-4-4-4-（羟基二苯甲基）-1-哌啶基]-1-氧代丁基]苯基]-2，2-二甲基乙酸甲酯（1），总收率约79％。该工艺反应条件温和，副反应少，易于操作，是一条适于工业化生产的合成路线。
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| 关 键 词： | 非索非那定 关键中间体 合成 |
Synthesis of a Key Intermediate of Fexofenadine |
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| Lu Xiao-yi,Wu Wen-liang,Dong Dao-min,Zhang Qi-ming.Synthesis of a Key Intermediate of Fexofenadine[J].Zhejiang Chemical Industry,2012,43(6):25-26. |
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| Authors: | Lu Xiao-yi Wu Wen-liang Dong Dao-min Zhang Qi-ming |
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| Affiliation: | (Zhejiang Qiming Pharmaceutical Co.,Ltd.,Shangyu,Zhejiang 312369,China) |
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| Abstract: | 2-4-4-4-(Hydroxydiphenylmethyl)-1-piperidinyl]-1-oxobutyl]phenyl]-2,2-dimethylacetic acid methyl ester was synthesized from methyl 4-(4-chloro-1-oxobutyl)-α,α-dimethylphenyl acetate with piperidine-4-carbonitrile to give methyl 2-(4-(4-(4-cyanopiperidin-1-yl)butanoyl)phenyl)-2-methylpropanoate,which was reacted with benzophenone and with an overall yield of 79%.This method is a suitable route for industrial manufacture with advantages of mild condition,few side reaction and easy operation. |
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| Keywords: | fexofenadine key intermediate synthesis |
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