State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences , 345 Lingling Road, Shanghai 200032, China.
J Am Chem Soc. 2014 Mar 5;136(9):3354-7. doi: 10.1021/ja412880r. Epub 2014 Feb 25.
A Cu(OAc)2-mediated C-H amidation and amination of arenes and heteroarenes has been developed using a readily removable directing group. A wide range of sulfonamides, amides, and anilines function as amine donors in this reaction. Heterocycles present in both reactants are tolerated, making this a broadly applicable method for the synthesis of a family of inhibitors including 2-benzamidobenzoic acids and N-phenylaminobenzoates.
一种使用易于去除的导向基团的 Cu(OAc)2 介导的芳基和杂芳基的 C-H 酰胺化和氨化反应已经被开发出来。在该反应中，各种磺酰胺、酰胺和苯胺都可以作为胺供体。反应物中存在的杂环也被容忍，这使得该方法在合成包括 2-苯甲酰胺苯甲酸和 N-苯基氨基苯甲酸酯在内的一系列抑制剂方面具有广泛的应用。
