Microwave-assisted synthesis of 3-substituted indoles via intramolecular arene-alkene coupling of o-iodoanilino enamines

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• 作者：Won-Il Lee ; Jong-Wha Jung ; Jaehoon Sim ; Hongchan An ; Young-Ger Suh
• 关键词：Indole ; Arene&ndash ; alkene coupling ; Microwave ; Enamine ; N ; O-Acetal TMS ether
• 刊名：Tetrahedron
• 出版年：2013
• 出版时间：2 September, 2013
• 年：2013
• 卷：69
• 期：35
• 页码：7211-7219
• 全文大小：709 K

文摘

A generally applicable and high-yielding protocol for the synthesis of 3-substituted indole derivatives is described. Key features include microwave-assisted intramolecular arene-alkene coupling of o-iodoanilino enamines, and expedient synthesis of o-iodoanilino enamine substrates employing N,O-acetal TMS ethers, which could be conveniently derived from the corresponding amides. Our unique procedure seems quite efficient and provides an easy access to a variety of 3-substituted indoles as privileged structure for a wide range of biological targets.