Mild and Efficient One-Pot Synthesis of 2-(Perfluoroalkyl)indoles by Means of Sequential Michael-Type Addition and Pd(II)-Catalyzed Cross-Dehydrogenative Coupling (CDC) Reaction

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• 作者：Dandan Shen ; Jing Han ; Jie Chen ; Hongmei Deng ; Min Shao ; Hui Zhang ; Weiguo Cao
• 刊名：Organic Letters
• 出版年：2015
• 出版时间：July 2, 2015
• 年：2015
• 卷：17
• 期：13
• 页码：3283-3285
• 全文大小：307K
• ISSN：1523-7052

文摘

2-Perfluoroalkylated indoles were efficiently synthesized via a one-pot cascade Michael-type addition/palladium-catalyzed intramolecular cross-dehydrogenative coupling (CDC) process, using molecular oxygen as the sole oxidant at 100 掳C in DMSO. This process allows atom economical assembly of indole rings from inexpensive and readily available anilines and methyl perfluoroalk-2-ynoates and tolerates a broad range of functional groups.