Mild Rh(III)-Catalyzed C鈥揌 Activation and Annulation with Alkyne MIDA Boronates: Short, Efficient Synthesis of Heterocyclic Boronic Acid Derivatives

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• 作者：Honggen Wang ; Christoph Grohmann ; Corinna Nimphius ; Frank Glorius
• 刊名：The Journal of the American Chemical Society
• 出版年：2012
• 出版时间：December 5, 2012
• 年：2012
• 卷：134
• 期：48
• 页码：19592-19595
• 全文大小：353K
• 年卷期：v.134,no.48(December 5, 2012)
• ISSN：1520-5126

文摘

Taking advantage of Rh(III)-catalyzed C鈥揌 activation reactions, we have developed a mild, short, and efficient method for the synthesis of bench-stable 3-isoquinolone MIDA boronates. The reaction is practical and scalable. The product formed has been applied in the Suzuki鈥揗iyaura reaction with high efficiency. This strategy has also been successfully expanded to the synthesis of MIDA boronate functionalized heterocycles such as isoquinoline, pyrrole, and indole.