Engineering Research Centre of Pharmaceutical Process Chemistry, Ministry of Education; School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, P.R. China.
Shanghai Jinli Pharmaceutical Co. Ltd., 108 Yuegong Road, Shanghai 201507, P.R. China.
J Org Chem. 2021 May 21;86(10):7296-7303. doi: 10.1021/acs.joc.1c00646. Epub 2021 May 5.
The direct arylation of aliphatic ketones has been developed via Pd-catalyzed β-C(sp)-H bond functionalization with 2-(aminooxy)-,-dimethylacetamide as a novel transient directing group (TDG), which showed remarkable directing ability to generate arylated products in moderate to good yields. Furthermore, the reaction can tolerate abundant substrate of ketones and aryl iodides. This study expands the scope of applications for TDGs.
通过钯催化的β-C(sp 3 )-H 键功能化反应,发展了脂肪族酮的直接芳基化反应,其中 2-(氨氧基)-,-二甲基乙酰胺作为一种新型的瞬态导向基团(TDG),具有显著的导向能力,可在中等至良好的收率下生成芳基化产物。此外,该反应可以耐受丰富的酮和芳基碘底物。这项研究扩展了 TDG 的应用范围。