化学
吲哚试验
丁二酰亚胺
马来酰亚胺
铑
组合化学
连接器
催化作用
点击化学
立体化学
作者
Hui‐Xiong Dai,Huiying Wang,mengmeng Wang,Biao Ma
出处
期刊:Synthesis
[Georg Thieme Verlag KG]
日期:2022-03-08
卷期号:54 (21): 4727-4733
摘要
Abstract Spiroindoles are key scaffolds in a large number of natural products, pharmaceuticals, and agrochemicals. Selective C–H activation has emerged as a powerful synthetic approach to streamline the synthesis of substituted spiroindoles. To date, various 2- and 3-indolyl-tethered aza-spiro-centers have been successfully achieved via C–H activation. However, introduction of spiro-containing systems onto the benzenoid core of indole still remains challenging. Herein, a method of Rh(III)-catalyzed selective C7-H activation/cyclization of indole with maleimide to afford novel spiroindole derivatives is reported, which incorporate both succinimide and spirocycle into indole unit. Gram-scale synthesis demonstrates the utility of this protocol, further modification via click chemistry offered a novel scaffold as a versatile spiro linker.
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