| (S)-和(R)-盐酸氟西汀的合成 |
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| 引用本文： | 陈国美,杨雪艳,奚倬勋,吴范宏.(S)-和(R)-盐酸氟西汀的合成[J].中国新药杂志,2007,16(22):1893-1895. |
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| 作者姓名： | 陈国美 杨雪艳 奚倬勋 吴范宏 |
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| 作者单位： | 华东理工大学结构可控先进材料教育部重点实验室,精细化学研究所,化学与分子工程学院,上海,200237 |
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| 摘 要： | 目的:研究光学活性盐酸氟西汀的合成工艺。方法:以苯乙酮为起始原料,经Mannich反应、还原、醚化3步反应合成外消旋氟西汀游离碱。外消旋体用L-( )-扁桃酸和D-(-)-扁桃酸反复交替拆分,分别得到了(S)-和(R)-型的盐酸氟西汀。结果:合成外消旋氟西汀游离碱的总收率为26.4%。拆分收率为42%。结论:该方法缩短了反应路线,操作简便,收率提高,适于工业生产。
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| 关 键 词： | 盐酸氟西汀 抗抑郁药 工艺改进 光学活性 |
| 文章编号： | 1003-3734（2007）22-1893-03 |
| 收稿时间： | 2006-08-10 |
| 修稿时间： | 2006年8月10日 |
Synthesis of (S)- and (R)-fluoxetine hydrochloride |
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| CHEN Guo-mei,YANG Xue-yan,XI Zhuo-xun,WU Fan-hong.Synthesis of (S)- and (R)-fluoxetine hydrochloride[J].Chinese Journal of New Drugs,2007,16(22):1893-1895. |
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| Authors: | CHEN Guo-mei YANG Xue-yan XI Zhuo-xun WU Fan-hong |
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| Abstract: | Objective: To study the synthesis of(S)-and(R)-fluoxetine hydrochloride.Methods: Fluoxetine was prepared using 1-phenylethanone as the starting material via four-step reaction,such as Mannich reaction,reduction and etherification etc.Separation of the(S)-and(R)-isomers of fluoxetine hydrochloride was realized through repeat-return separation method using L-( )-and D-(-)-madelic acid.Results: Fluoxetine was synthesized from 1-phenylethanone in the overall yield of 26.4%.The resolution yield was 42%.Conclusion: The process is a good method for pharmaceutical manufacture. |
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| Keywords: | fluoxetine hydrochloride antidepressive drug process improvement optical activity |
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