Department of Chemistry, School of Science, Xi'an Key Laboratory of Sustainable Energy Materials Chemistry, and MOE Key Laboratory for Nonequilibrium Synthesis and Modulation of Condensed Matter , Xi'an Jiaotong University , Xi'an 710049 , China.
J Org Chem. 2019 Jul 5;84(13):8615-8629. doi: 10.1021/acs.joc.9b01084. Epub 2019 Jun 20.
The efficient copper-catalyzed cyanoalkylation of amines via C-C bond cleavage has been demonstrated. Distinctive features of this procedure involves mild conditions, broad range of nitrogen nucleophiles, high selectivity, and good functional group tolerance, thus providing a useful approach for the C(sp)-N bond formations. Most importantly, this protocol is applicable to the late-stage functionalization of natural products, amino acid esters, and drugs. Mechanistic studies suggest that a radical intermediate was involved in this transformation.
通过 C-C 键断裂实现了高效的铜催化胺的氰基烷基化反应。该方法的显著特点是反应条件温和、氮亲核试剂适用范围广、选择性高、官能团容忍性好，为 C(sp)-N 键的形成提供了一种有用的方法。最重要的是，该方案适用于天然产物、氨基酸酯和药物的后期官能团化。机理研究表明，该转化涉及自由基中间体。
