中华医学超声杂志

应用化学 ›› 2010, Vol. 27 ›› Issue (04): 494-496.DOI: 10.3724/SP.J.1095.2010.90420

• 研究简报 • 上一篇    

5-甲基-2，3-二苯基-1，5-苯并硫氮杂卓-4(5H)-酮的合成

陶李明1*,刘文奇1,谭倪2,周芸1   

  1. (1.湘南学院化学与生命科学系 郴州 423000；2.南华大学化学化工学院 衡阳)
  • 收稿日期:2009-06-24 修回日期:2009-07-28 出版日期:2010-04-10 发布日期:2010-04-10
  • 通讯作者: 陶李明，女，副教授; E-mail:taoliming2005@yahoo.com.cn; 研究方向：有机催化合成
  • 基金资助:
    湖南省自然科学基金（08JJ3018）湖南省教育厅(08C828）资助项目

Synthesis of 5-Methyl-2,3-diphenyl-1,5-benzothiazepin-4(5H)-one

TAO Li-Ming1*, LIU Wen-Qi1, TAN Ni2, ZHOU Yun1   

  1. (1.Department of Chemistry and Life Science,Xiangnan University,Chenzhou 423000;
    2.School of Chemistry and Chemical Engineering,University of South China,Hengyang)
  • Received:2009-06-24 Revised:2009-07-28 Published:2010-04-10 Online:2010-04-10

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摘要：

以2-甲硫基苯胺为原料，通过酰化、碘环化以及Suzuki交叉偶联反应，合成了5-甲基-2，3-二苯基-1，5-苯并硫氮杂卓-4(5H)-酮。 分别考察了催化剂对酰化反应、溶剂对碘环化反应的影响，以及催化剂、配体、碱和温度等因素对Suzuki交叉偶联反应的影响，在最佳的反应条件下，反应总收率为68.5%，中间产物和目标产物的结构经IR、NMR和MS等测试技术得以确证。

关键词: 甲基二苯基苯并硫氮杂卓-4(5H)-酮, 酰化反应, 碘环化反应, Suzuki交叉偶联反应

Abstract:

5-Methyl-2,3-diphenyl-1,5-benzothiazepin-4(5H-)-one was synthesized via the acylation reaction and iodocyclization reaction and Suzuki cross-coupling reaction with 2-(methylthio)aniline as the initial material. Effects including catalysts on acylation reaction, solvents on iodocyclization and catalysts, ligand, base and reaction temperature on Suzuki cross-coupling reaction have been investigated. Under optimum conditions, the yield of the product was up to 68.5%. The chemical structures of the intermediates and target product were characterized by IR, NMR and MS spectra.

Key words: Methyldiphenylbenzothiazepin-4(5H)-one, acylation reaction, iodocyclization, Suzuki cross-coupling reaction

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