State Key Laboratory of Natural Medicines and Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, PR China.
Chem Commun (Camb). 2012 Apr 18;48(31):3763-5. doi: 10.1039/c2cc00081d. Epub 2012 Mar 8.
The first palladium-catalyzed direct C5-arylation of azole-4-carboxylates with simple unactivated arenes through double C-H bond cleavage is realized. This protocol provided a straightforward access to diverse 5-arylsubstituted azole-4-carboxylic derivatives with good functional group tolerance.
首次实现了钯催化唑-4-羧酸酯与简单未活化芳基的直接 C5-芳基化反应,通过双 C-H 键断裂。该方案为具有良好官能团耐受性的各种 5-芳基取代唑-4-羧酸衍生物提供了直接途径。