Department of Chemistry, Indiana University, 800 East Kirkwood Avenue, Bloomington, Indiana 47405-7102, United States.
J Org Chem. 2023 Apr 7;88(7):4757-4760. doi: 10.1021/acs.joc.2c02461. Epub 2023 Mar 13.
Herein, we describe a formal dehydrogenative cross coupling of heterocycles with unactivated aliphatic amines. The resulting transformation enables the direct alkylation of common heterocycles by merging N-F-directed 1,5-HAT with Minisci chemistry, leading to predictable site selectivity. The reaction provides a direct route for the transformation of simple alkyl amines to value-added products under mild reaction conditions, making this an attractive option for C(sp)-H heteroarylation.
在此，我们描述了杂环化合物与未活化脂肪族胺的脱氢交叉偶联。这种转化通过将 N-F 导向的 1,5-HAT 与 Minisci 化学合并，实现了常见杂环的直接烷基化，从而产生可预测的位点选择性。该反应在温和的反应条件下为简单的烷基胺转化为增值产品提供了直接途径，这使得 C(sp)-H 杂芳基化成为一种有吸引力的选择。
