A Practical Synthesis of Indoles via a Pd-Catalyzed C鈥揘 Ring Formation
详细信息 查看全文
- 作者：Rishi G. Vaswani ; Brian K. Albrecht ; James E. Audia ; Alexandre C么t茅 ; Les A. Dakin ; Martin Duplessis ; Victor S. Gehling ; Jean-Christophe Harmange ; Michael C. Hewitt ; Yves Leblanc ; Christopher G. Nasveschuk ; Alexander M. Taylor
- 刊名：Organic Letters
- 出版年：2014
- 出版时间：August 15, 2014
- 年：2014
- 卷：16
- 期：16
- 页码：4114-4117
- 全文大小：290K
- ISSN：1523-7052
文摘
A method for the synthesis of N-functionalized C2-/C3-substituted indoles via Pd-catalyzed C鈥揘 bond coupling of halo-aryl enamines is described. The general strategy utilizes a variety of amines and 尾-keto esters which are elaborated into halo-aryl enamines as latent precursors to indoles. The preferred conditions comprising the RuPhos precatalyst and RuPhos in the presence of NaOMe in 1,4-dioxane tolerate a variety of substituents and are scalable for the construction of indoles in multigram quantities.