Key Laboratory of Ministry of Education for Advanced Materials in Tropical Island Resources, Hainan Provincial Key Lab of Fine Chemicals, Hainan Provincial Fine Chemical Engineering Research Center, Hainan University, Haikou 570228, China.
Org Lett. 2020 Jul 17;22(14):5517-5521. doi: 10.1021/acs.orglett.0c01869. Epub 2020 Jun 30.
A palladium-catalyzed N-acylation of tertiary amines by carboxylic acids was achieved through C-N cleavage. This reaction showed a wide substrate scope. Both aromatic and aliphatic acids served well as the acylating reagents and coupled with tertiary amines to produce the corresponding amides in good to excellent yields. With the strategy, bioactive carboxylic acids were also efficiently modified, highlighting the synthetic value of the process in organic synthesis.
钯催化的羧酸对叔胺的 N-酰化反应通过 C-N 键的断裂实现。该反应具有广泛的底物范围。芳香酸和脂肪酸都可以作为酰化试剂，与叔胺反应，以良好到优秀的收率得到相应的酰胺。利用该策略，还可以有效地修饰生物活性羧酸，突出了该过程在有机合成中的合成价值。
