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

作者：Lee Won Il; Jung Jong Wha; Sim Jaehoon; An Hongchan; Suh Young Ger^*

来源：Tetrahedron, 2013, 69(35): 7211-7219.

DOI：10.1016/j.tet.2013.06.101

• Indole
• Arene-alkene coupling
• Microwave
• Enamine
• N,O-Acetal TMS ether

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.

• 出版日期2013-9-2