Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (12): 3242-3249.DOI: 10.6023/cjoc201806039 Previous Articles     Next Articles



白丽丽, 王颖, 王烁今, 孔杜林, 付艳, 彭德乾, 文丽君, 陈训   

  1. 海南医学院药学院 海口 571199
  • 收稿日期:2018-06-25 修回日期:2018-07-23 发布日期:2018-08-23
  • 通讯作者: 彭德乾, 陈训;
  • 基金资助:


Ruthenium(Ⅱ)-Catalyzed C-H Bond Regioselective[3+2] Annulation of Arylamines with Propargyl Alcohols

Bai Lili, Wang Ying, Wang Shuojin, Kong Dulin, Fu Yan, Peng Deqian, Wen Lijun, Chen Xun   

  1. School of Pharmacy, Hainan Medical University, Haikou 571199
  • Received:2018-06-25 Revised:2018-07-23 Published:2018-08-23
  • Contact: 10.6023/cjoc201806039;
  • Supported by:

    Project supported by the Program of Hainan Association for Science and Technology Plans to Youth R & D Innovation (Nos. QCXM201808, QCXM201707).

A simple and efficient ruthenium(Ⅱ)-catalyzed C-H bond regioselective[3+2] annulation of arylamines with propargyl alcohols has been reported. This protocol provides a facile approach to hydroxy-containing indole skeleton, which could be employed for constructing more complex and useful pharmaceutical molecules. Meantime, the kinetic isotope effect was further investigated and the results indicated that the C-H bond-breaking was possibly involved in the rate-limiting step of this transformation.

Key words: ruthenium(Ⅱ), C-H bond, regioselective, annulation reaction