Regioselective Palladium-Catalyzed Arylation of 4-Chloropyrazoles

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• 作者：Carlos Mateos ; Javier Mendiola ; Mercedes Carpintero ; Jos Miguel Mnguez
• 刊名：Organic Letters
• 出版年：2010
• 出版时间：November 5, 2010
• 年：2010
• 卷：12
• 期：21
• 页码：4924-4927
• 全文大小：264K
• 年卷期：v.12,no.21(November 5, 2010)
• ISSN：1523-7052

文摘

A highly regioselective Pd-catalyzed arylation of N-methylpyrazoles with aryl bromides is described. This transformation was studied extensively via automated reaction screening. A Design of Experiments (DoE) approach for optimizing the critical parameters was applied, resulting in excellent conditions for preparing selectively 5-arylpyrazoles in moderate to excellent yields under mild conditions.