School of Chemical and Biological Engineering, University of Science and Technology Beijing, Beijing 100083, P. R. China.
Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, P. R. China.
J Org Chem. 2022 May 6;87(9):5543-5555. doi: 10.1021/acs.joc.1c02868. Epub 2022 Apr 13.
Using -methoxyamide reagents as an amide source, C-H amidation was realized at the ortho position of azine under the action of rhodium and boric acid. The method has mild reaction conditions, high atomic utilization, excellent yield, and wide adaptability to amidation reagents (both aromatic amides and fatty amides are applicable). Amide-substituted ketones can be obtained by a simple treatment and can be further transformed into bioactive substances. This provides a good supplement for the C-H bond amidation of aromatic rings.
使用 -methoxyamide 试剂作为酰胺源，在铑和硼酸的作用下，嗪的邻位实现了 C-H 酰胺化。该方法具有反应条件温和、原子利用率高、产率优异、酰胺化试剂适应性广（芳酰胺和脂肪酰胺均可适用）的特点。通过简单的处理可以得到酰胺取代的酮，并且可以进一步转化为生物活性物质。这为芳环的 C-H 键酰胺化提供了很好的补充。
