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4—(3,4—二氯苯基)—3,4—二氢—1(2H)—萘酮的合成

Synthesis of Intermediate 4—(3,4—Dichlorophenyl)—1—Tetralone
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摘要 邻二氯苯和丁二酸酐经付-克酰化制得,再经还原、付-克酰化和闭环等反应得到抗抑郁剂舍曲林的中间体4-(3,4-二氯苯基)-3,4-二氢-1(2H)-萘酮,总收率50%。第1步反应n(AlCl3):n(丁二酸酐)=2.2:1较为适宜。 4- (3,4- dichlorophenyl)- 1- tetralone was synthesized in an ov erall yield 50% from o- dichlorobenzene and succinicanhydride as raw materials through Frield- Crafts acylation reaction , followed by chemical reduction, Frield- Crafts acylation, cyclization.
作者 谢建伟 蒋祖林 陈俊
机构地区 衢州学院(筹)化学与制药工程系 浙江中贝九州集团有限公司 浙江工程设计有限公司
出处 《化工生产与技术》 CAS 2005年第4期42-43,共2页 Chemical Production and Technology
关键词 4-(3 4-二氯苯基)-3 4-二氢-1(2H)-萘酮 合成方法 产品收率 抗抑郁药 医药 舍曲林 sertraline antidepressant 4- (3,4- dichlorophenyl)- 1- tetra lone
分类号 TQ244.3 [化学工程—有机化工]
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参考文献5

  • 1文熙,胡惟孝,杨忠愚.抗抑郁药舍曲林的合成进展[J].合成化学,2003,11(5):391-398. 被引量：8
  • 2孙乐盈,虞心红,张昊,王建兵,吴达俊.盐酸舍曲林的合成路线图解[J].中国医药工业杂志,2004,35(9):569-571. 被引量：4
  • 3George J Quallich, Michael T williams. Process for preparing sertraline from chiraltetraline : US, 4839104 [ P]. 1989 - 06 -13.
  • 4Geraldine P Taber, David M Pfisterer, Juan C. Colberg A New and Simplified Process for Preparing N - [4 - (3, 4 -Dichlorophenyl) - 3, 4 - dihydro - 1 (2 H) - naphthalenyl -idene]methanamine and a Telescoped Process for theSynthesis of ( IS - cis) - 4 - (3, 4 - Dichlorophenol) - 1, 2,3, 4 - tetrahydro - N - methyl - 1 - naphthalenamine Mandelate: Key Intermediates in the Synthesis of Sertraline Hydrochloride [ J ]. Organic Process Research & Development,2004, 8(3), 385 - 388.
  • 5Guy P. Adrian. Method of Preparing 4 - dichlorophenyl - 1 -tetralones: US, 5019655 [P]. 1991 - 05 - 28.

二级参考文献45

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化工生产与技术
2005年 第4期

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