Synthesis of Chiral Piperazines via Hydrogenation of Pyrazines Activated by Alkyl Halides

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• 作者：Wen-Xue Huang ; Lian-Jin Liu ; Bo Wu ; Guang-Shou Feng ; Baomin Wang ; Yong-Gui Zhou
• 刊名：Organic Letters
• 出版年：2016
• 出版时间：July 1, 2016
• 年：2016
• 卷：18
• 期：13
• 页码：3082-3085
• 全文大小：350K
• 年卷期：0
• ISSN：1523-7052

文摘

A facile method has been developed for the synthesis of chiral piperazines through Ir-catalyzed hydrogenation of pyrazines activated by alkyl halides, giving a wide range of chiral piperazines including 3-substituted as well as 2,3- and 3,5-disubstituted ones with up to 96% ee. The high enantioselectivity, easy scalability, and concise drug synthesis demonstrate the practical utility.