College of Chemistry and Pharmaceutical Sciences, Qingdao Agricultural University , Qingdao 266109, China.
J Org Chem. 2017 Aug 18;82(16):8703-8709. doi: 10.1021/acs.joc.7b00732. Epub 2017 Aug 1.
The first transition-metal free and regioselective C(sp)-H arylation of 2-alkylazaarenes with nitroarenes has been achieved via t-BuOK-mediated dehydrogenative C(sp)-C(sp) coupling. This reaction provides an efficient access to the biologically important and synthetically useful 2-benzyl-substituted azaarenes under mild conditions without the need of prefunctionalization of 2-alkylazaarenes or using the specialized arylating agents.
首次实现了无过渡金属和区域选择性的 2-烷基氮杂芳烃与硝基芳烃的 C(sp)-H 芳基化反应,该反应通过 t-BuOK 介导的脱氢 C(sp)-C(sp) 偶联实现。在温和条件下,该反应无需对 2-烷基氮杂芳烃进行预官能化或使用特殊的芳基化试剂,为具有重要生物学意义和合成价值的 2-苄基取代氮杂芳烃提供了一种有效的合成方法。