Department of Chemistry, Emory University, Atlanta, Georgia 30322, United States.
Loxo Oncology, Boulder, Colorado 80301, United States.
Org Lett. 2023 Mar 10;25(9):1397-1402. doi: 10.1021/acs.orglett.3c00126. Epub 2023 Feb 27.
Here, we report an efficient and modular approach toward the formation of difluorinated arylethylamines from simple aldehyde-derived -dialkylhydrazones and trifluoromethylarenes (CF-arenes). This method relies on selective C-F bond cleavage via reduction of the CF-arene. We show that a diverse set of CF-arenes and CF-heteroarenes react smoothly with a range of aryl and alkyl hydrazones. The β-difluorobenzylic hydrazine product can be selectively cleaved to form the corresponding benzylic difluoroarylethylamines.
在这里,我们报告了一种从简单的醛衍生的二烷基腙和三氟甲基芳烃(CF-芳烃)形成二氟芳基乙胺的有效和模块化方法。该方法依赖于通过还原 CF-芳烃选择性地裂解 C-F 键。我们表明,一系列不同的 CF-芳烃和 CF-杂芳烃与各种芳基和烷基腙反应顺利。β-二氟苄基腙产物可以选择性地裂解,形成相应的苄基二氟芳基乙胺。