Chin. J. Org. Chem. ›› 2013, Vol. 33 ›› Issue (03): 630-633.DOI: 10.6023/cjoc201210038 Previous Articles     Next Articles



程绎南, 谢桂英, 孙淑君, 游秀峰   

  1. 河南农业大学植保学院 郑州 450002
  • 收稿日期:2012-10-19 修回日期:2012-12-05 发布日期:2012-12-20
  • 通讯作者: 程绎南

A Practical Synthesis of 3-{[4-(2,6-Dichlorophenyl)piperidin-1-yl]- methyl}-2-(thiophen-2-yl)-1H-indole as a New Ligand for Opioid Receptor Like 1 Receptor

Cheng Yinan, Xie Guiying, Sun Shujun, You Xiufeng   

  1. Plant Protection College, Henan Agricultural University, Zhengzhou 450002
  • Received:2012-10-19 Revised:2012-12-05 Published:2012-12-20

3-{[4-(2,6-Dichlorophenyl)piperidin-1-yl]methyl}-2-(thiophen-2-yl)-1H-indole (1) as a ligand for opioid receptor like 1 receptor was prepared via four steps from commercially available phenylhydrazine (2), 1-(thiophen-2-yl)- ethanone (3), 2,6-dichloro- phenyl-boronic acid (5) and 4-bromopyridine (6). This convenient approach was green and had potential application for the scale production because of recoverable reaction medium, simple isolating process of intermedi-ates, little waste and highly total yield of 65%.

Key words: substituted indole, synthesis, catalytic hydrogenation, condensation