Negishi Approach to 1,5-Disubstituted 3-Amino-1H-1,2,4-triazoles

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• 作者：Jeff Shen ; Brian Wong ; Chunang Gu ; Haiming Zhang
• 刊名：Organic Letters
• 出版年：2015
• 出版时间：October 2, 2015
• 年：2015
• 卷：17
• 期：19
• 页码：4678-4681
• 全文大小：303K
• ISSN：1523-7052

文摘

An efficient synthesis of 1,5-disubstituted 3-amino-1H-1,2,4-triazoles has been achieved via a Negishi coupling of aryl or vinyl bromides and 1-substituted 3-amino-1H-1,2,4-triazoles in the presence of Knochel鈥檚 base tetramethylpiperidinylzinc chloride lithium chloride (TMPZnCl路LiCl) and catalytic bis(di-tert-butylphenylphosphine)palladium chloride. This chemistry tolerates a variety of electronically diverse aryl or vinyl bromides and 1-substituted 3-amino-1H-1,2,4-triazoles.