Copper-Catalyzed Oxidative Diamination of Terminal Alkynes by Amidines: Synthesis of 1,2,4-Trisubstituted Imidazoles

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• 作者：Jihui Li ; Luc Neuville
• 刊名：Organic Letters
• 出版年：2013
• 出版时间：April 5, 2013
• 年：2013
• 卷：15
• 期：7
• 页码：1752-1755
• 全文大小：276K
• 年卷期：v.15,no.7(April 5, 2013)
• ISSN：1523-7052

文摘

An efficient copper-catalyzed synthesis of 1,2,4-trisubstituted imidazoles using amidines and terminal alkynes has been developed. Overall, the oxidative process, which involves Na₂CO₃, pyridine, a catalytic amount of CuCl₂路2H₂O, and oxygen (1 atm), consisted of a regioselective diamination of alkynes allowing the synthesis of diverse imidazoles in modest to good yields.