Palladium-Catalyzed Remote C(sp3)鈥揌 Arylation of 3-Pinanamine

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• 作者：Wei Cui ; Shengwei Chen ; Jia-Qiang Wu ; Xin Zhao ; Wenhui Hu ; Honggen Wang
• 刊名：Organic Letters
• 出版年：2014
• 出版时间：August 15, 2014
• 年：2014
• 卷：16
• 期：16
• 页码：4288-4291
• 全文大小：342K
• ISSN：1523-7052

文摘

3-Pinanamine is a prevalent motif in medicinal chemistry and asymmetric synthesis. In line with the pursuit of novel 3-pinanamine based anti-influenza virus A agent, the direct functionalization of 3-pinanamine was achieved by using Pd-catalyzed C(sp³)鈥揌 activation logic. Good substrate scope and functional group tolerance were observed. The reaction represents a rare example of a direct functionalization of an aliphatic amine at the remote 未 position.