二氯双(4-甲基异丙基苯基)钌(II)二聚体催化N-(2-吡啶基)-吲哚与查尔酮Micheal加成反应研究

[RuCl_(2)(p-cymene)]_(2)-catalyzed Micheal addition reaction of N-(2-pyridyl)indoles with chalcones

研究了[RuCl_(2)(p-cymene)]2催化N-(2-吡啶基)吲哚与查尔酮的碳氢键活化Micheal加成反应。通过考察溶剂及添加剂,确定了最佳的反应条件:N-(2-吡啶基)吲哚与查尔酮摩尔比为1∶3,在1,2-二氯乙烷溶剂中加热至80℃,反应12 h,可获得收率为85%的模板产物。在最佳的反应条件下,合成了一系列含3位取代吲哚的黄酮类化合物,收率为65%~85%。结果表明,该方法反应条件温和,高效可控,具有良好的官能团耐受性。

A[RuCl_(2)(p-cymene)]_(2)-catalyzed novel Micheal addition method of N-(2-pyridyl)indoles with chalcones was investigated.According to our screening of reaction parameters,the optimized conditions were determined by screening the solvent,reaction temperature and additive,involving:the ratio of N-(2-pyridyl)indoles and chalcones(1∶3)in DCE at 80℃with a reaction time of 12 h,giving the model product in 85%yield.Having established the optimal reaction conditions,a range of N-(2-pyridyl)indoles and chalcones were producted,affording the corresponding products in 65%-85%yields.The results show that the reaction condition of this method is mild,efficient and controllable,and it has good functional group tolerance.