Department of Organic Chemistry, College of Chemistry, Jilin University, 2699 Qianjin Street, Changchun 130012, P. R. China.
State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, P. R. China.
Org Lett. 2021 Dec 17;23(24):9591-9596. doi: 10.1021/acs.orglett.1c03802. Epub 2021 Dec 7.
A copper-catalyzed difluoroalkylation of an alkene/nitrile insertion/cyclization tandem sequence of -cyanamide alkene was described, which provided a convenient synthetic approach for accessing difluorinated bicyclic amidines bearing imine moieties in a sustainable fashion. This protocol is characterized by high yields, a broad substrate scope, and good functional group compatibility. In addition, the desired product can be readily converted into other valuable functionalized fluorinated aza-heterocycles.
描述了铜催化的烯烃/腈插入/环化串联序列的二氟烷基化反应，-氰基烯烃，为可持续地获得含亚胺部分的二氟双环脒提供了一种方便的合成方法。该方案具有收率高、底物范围广、官能团兼容性好等特点。此外，所需产物可容易地转化为其他有价值的氟化氮杂环化合物。
