Synthesis of Azepino[4,5-b]indole via Ring Expansion of Tetrahydro-β-carbolines Ammonium Ylide,The Journal of Organic Chemistry

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Synthesis of Azepino[4,5-b]indole via Ring Expansion of Tetrahydro-β-carbolines Ammonium Ylide
The Journal of Organic Chemistry ( IF 3.3 ) Pub Date : 2023-12-29 , DOI: 10.1021/acs.joc.3c02249
Wang Shen ₁ , Xiyao Lu ₁ , Yu Shen ₁ , Junjian Li ₁ , Aiqun Jia ₂ , Shi Tang ₁

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The formal cyclization strategy was generally used to construct azepino[4,5-b]indole. Herein, we reported a novel and expeditious protocol for the synthesis of quaternary carbon azepino[4,5-b]indole via ring expansion of ammonium ylide, which was formed by the reaction of tetrahydro-β-carbolines with the diazo compound. The easily available substrates, mild reaction conditions, and broad functional tolerance rendered this method a practical strategy that may significantly afford an efficient method of scaffold hopping in drug discovery.

中文翻译：

四氢-β-咔啉铵叶立德扩环合成氮杂[4,5-b]吲哚

正式的环化策略通常用于构建氮杂[4,5- b ]吲哚。在此，我们报道了一种通过四氢-β-咔啉与重氮化合物反应形成的铵叶立德扩环合成季碳氮杂[4,5- b ]吲哚的新颖且快速的方案。易于获得的底物、温和的反应条件和广泛的功能耐受性使该方法成为一种实用策略，可以在药物发现中显着提供有效的支架跳跃方法。

更新日期：2023-12-29

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