Highly Regioselective N-2 Arylation of 4,5-Dibromo-1,2,3-triazole: Efficient Synthesis of 2-Aryltriazoles

被引：83

作者：

Wang, Xiao-jun ^{[1
]}

Zhang, Li ^{[1
]}

Lee, Heewon ^{[1
]}

Haddad, Nizar ^{[1
]}

Krishnamurthy, Dhileepkumar ^{[1
]}

Senanayake, Chris H. ^{[1
]}

机构：

[1] Boehringer Ingelheim Pharmaceut Inc, Dept Chem Dev, Ridgefield, CT 06877 USA

来源：

ORGANIC LETTERS | 2009年 / 11卷 / 21期

关键词：

CLICK CHEMISTRY; CYCLOADDITION;

D O I：

10.1021/ol9019875

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Reaction of 4,5-dibromo-1,2,3-triazole with electron-deficient aromatic halides in the presence of potassium carbonate in DMF produces the corresponding 2-aryl-4,5-dibromotriazoles with high regioselectivity. Subsequent debromination of these triazoles by hydrogenation furnishes 2-aryltriazoles in excellent yields. Overall, this two-step process provides an efficient access to 2-aryl-1,2,3-triazoles.

引用

页码：5026 / 5028

页数：3

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