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Palladium-Catalyzed Late-Stage Direct Arene Cyanation
Chem ( IF 23.5 ) Pub Date : 2018-11-01 , DOI: 10.1016/j.chempr.2018.09.027
Da Zhao , Peng Xu , Tobias Ritter

Methods for direct benzonitrile synthesis are sparse, despite the versatility of cyano groups in organic synthesis and the importance of benzonitriles for the dye, agrochemical, and pharmaceutical industries. We report the first general late-stage aryl C–H cyanation with broad substrate scope and functional-group tolerance. The reaction is enabled by a dual-ligand combination of quinoxaline and an amino acid-derived ligand. The method is applicable to direct cyanation of several marketed small-molecule drugs, common pharmacophores, and organic dyes.



中文翻译:

钯催化后期直接芳烃氰化

尽管氰基在有机合成中具有多功能性,并且苯甲腈在染料,农业化学和制药行业中的重要性,但直接合成苯甲腈的方法仍然很少。我们报告了第一个一般的晚期芳基C–H氰化反应,具有较宽的底物范围和官能团耐受性。喹喔啉和氨基酸衍生的配体的双配体结合使反应得以实现。该方法适用于几种市售的小分子药物,常用药效团和有机染料的直接氰化。

更新日期:2018-11-01
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