张珉教授课题组
祝贺曹梁成果发表于《Nat. Commun.》
发布时间: 2021-08-01 浏览次数: 55

祝曹梁同学在《Nat. Commun.》上发表研究论文

Practical Iridium-Catalyzed Direct α-arylation of N-heteroarenes with (Hetero)arylboronic Acids by H2O-Mediated H2 Evolution

Liang Cao,1 He Zhao,1 Rongqing Guan,1 Huanfeng Jiang,1 and Min Zhang1,*

ABSTRACT:Despite the widespread applications of 2-(hetero)aryl N-heteroarenes in numerous fields of science and technology, universal access to such compounds is easily hampered due to the lack of a general method for their synthesis. Herein, by a H2O-mediated H2-evolution cross-coupling strategy, we report a new iridium(III)-catalyzed facile method to direct α-arylation of N-heteroarenes with both aryl and heteroaryl boronic acids, proceeding with broad substrate scope and excellent functional compatibility, oxidant and reductant-free conditions, operational simplicity, easy scalability, and no need for prefunctionalization of N-heteroarenes. This method offers applicability for structural modification of biomedical molecules, but also a practical route for direct access to 2-(hetero)aryl N-heteroarenes, a class of potential cyclometalated C^N ligands and N^N bidentate ligands that are difficult to prepare with the existing α-C-H arylation methods, thus filling an important gap in the capabilities of synthetic organic chemistry.

Nat. Commun., 2021, DOI:10.1038/s41467-021-01378-3