摘要/Abstract
报道了一种简便有效的Ru(Ⅱ)-催化芳胺C-H键与炔丙醇的高选择性[3+2]环化反应,能够高效构建含有羟基功能基的吲哚骨架结构,为进一步衍生更加复杂有用的药物分子提供简便的合成渠道.同时研究了该反应的动力学同位素效应,实验结果表明C-H键活化可能属于整个反应历程的决速步骤.
关键词: 钌(Ⅱ), C-H键, 高选择性, 环化反应
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
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