| (S)-1-(1-苯基乙基)-4-哌啶酮的合成 |
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| 引用本文： | 王娟,李美玲,陈立功,李阳,闫喜龙,王东华.(S)-1-(1-苯基乙基)-4-哌啶酮的合成[J].精细化工,2007,24(11):1109-1111. |
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| 作者姓名： | 王娟 李美玲 陈立功 李阳 闫喜龙 王东华 |
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| 作者单位： | 1. 天津大学,药物科学与技术学院,天津,300072
2. 天津大学,化工学院,天津,300072 |
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| 摘 要： | 该文以(S)-1-苯乙胺、丙烯酸甲酯为原料,经Michael加成,Dieckmann环合,脱羧,合成了(S)-1-(1-苯基乙基)-4-哌啶酮。并对所涉及的Michael加成反应的工艺参数进行了优化。当(S)-1-苯乙胺与丙烯酸甲酯的摩尔比为1∶2.5,40℃反应10h,收率为92.4%,总收率为89.3%。目标产物及中间体的结构经核磁共振波谱进行了表征。
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| 关 键 词： | 哌啶酮 Michael加成 Dieckmann环合 脱羧 药物中间体 |
| 文章编号： | 1003-5214（2007）11-1109-03 |
| 修稿时间： | 2007-03-23 |
Synthesis of (S)-1-(1-Phenylethyl)-4-piperidone |
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| WANG Juan,LI Mei-ling,CHEN Li-gong,LI Yang,YAN Xi-long,WANG Dong-hua.Synthesis of (S)-1-(1-Phenylethyl)-4-piperidone[J].Fine Chemicals,2007,24(11):1109-1111. |
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| Authors: | WANG Juan LI Mei-ling CHEN Li-gong LI Yang YAN Xi-long WANG Dong-hua |
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| Affiliation: | 1. School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, China ; 2. School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China |
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| Abstract: | (S)-1-(1-Phenylethyl)-4-piperidone(Ⅰ) was prepared from (S)-1-phenylethylamine and methyl acrylate through Michael addition,Dieckmann cyclization and decarboxylation.Technological parameters involved in Michael addition were optimized.Thus,(S)-1-phenylethylamine reacted with methyl acrylate in mole ratio 1∶2.5 under 40 ℃ for 10 h to give the intermediate in 92.4% yield,and the total yield of Ⅰ was 89.3%.Structures of the title compound and the intermediate were confirmed by 1HNMR and 13CNMR. |
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| Keywords: | piperidone Michael addition Dieckmann cyclization decarboxylation drug intermediates |
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