| N,N-二甲基-3-羟基-3-(2-噻吩基)丙胺的合成与拆分 |
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| 引用本文： | 郭莉娜,侯仲轲,李宏伟,陈灿. N,N-二甲基-3-羟基-3-(2-噻吩基)丙胺的合成与拆分[J]. 精细化工中间体, 2007, 37(2): 42-43,51 |
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| 作者姓名： | 郭莉娜 侯仲轲 李宏伟 陈灿 |
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| 作者单位： | 1. 华中师范大学,化学学院,湖北,武汉,430079
2. 湖南化工研究院,药物研究所,湖南,长沙,410007 |
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| 摘 要： | 以2-乙酰噻吩、多聚甲醛、二甲胺盐酸盐为起始原料合成3-二甲胺基-1-(2-噻吩基)-1-丙酮盐酸盐,然后经硼氢化钠还原,(S)-(+)-扁桃酸拆分,得到(S)-N,N-二甲基-3-羟基-3-(2-噻吩基)丙胺,总收率38.8%,e.e值95.6%。回收的扁桃酸可再应用于拆分。
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| 关 键 词： | (S)-N,N-二甲基-3-羟基-3-(2-噻吩基)丙胺 (S)-(+)-扁桃酸 拆分 |
| 文章编号： | 1009-9212（2007）02-0042-02 |
| 修稿时间： | 2007-01-09 |
Synthesis and Resolution of N,N-Dimethyl-3-(2-thienyl)-3-bydroxypropanamine |
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| GUO Li-na,HOU Zhong-ke,LI Hong-wei,CHEN Can. Synthesis and Resolution of N,N-Dimethyl-3-(2-thienyl)-3-bydroxypropanamine[J]. Fine Chemical Intermediates, 2007, 37(2): 42-43,51 |
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| Authors: | GUO Li-na HOU Zhong-ke LI Hong-wei CHEN Can |
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| Affiliation: | 1. Department of Chemistry, Central China Normal University, Wuhan 430079, China; 2. Hunan Research Institute of MateriaMedica, Changsha 410007, China |
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| Abstract: | 2-Thienyl-3-dimethylaminoethyl ketone hydrochloride was synthesized from 1-(thiophen-2-yl)-ethanone,dimethylamine hydrochloride and paraformaldehyde.(S)-N,N-dimethyl-3-(2-thienyl)-3-hydroxypropanamine was obtained by reduction of 2-thienyl-2-dimethylaminoethyl ketone hydrochloride by NaBH4,and resolution by (S)-( )-mandelic acid in 38.8% yield. Enantiomers of (S)-N,N-dimethyl-3-(2-thienyl)-3-hydroxypropanamine was 95.6%. (S)-( )-mandelic acid could be reused. |
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| Keywords: | (S)-N N-dimethyl-3-(2-thienyl)-3-hydroxypropanamine (S)-( )-mandelic acid resolution |
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