Zhao Jiajun, Wang Jianwei, Wang Shangyuan, Ying Jun
School of Chemistry and Chemical Engineering, Key Laboratory of Surface & Interface Science of Polymer Materials of Zhejiang Province, Zhejiang Sci-Tech University, Hangzhou 310018, China.
Zhejiang Sci-Tech University, Shengzhou Innovation Research Institute, Shengzhou 312400, China.
J Org Chem. 2024 Oct 4;89(19):14505-14509. doi: 10.1021/acs.joc.4c01032. Epub 2024 Sep 17.
A Cu/Pd-catalyzed tandem radical cyclization and carbonylation of alkyne-tethered α-bromocarbonyls with phenols has been developed for the expedited construction of ester-containing 3,4-dihydroquinolin-2(1)-one scaffolds. By employing benzene-1,3,5-triyl triformate (TFBen) as the CO source, the reaction proceeded smoothly to afford a series of ester-containing 3,4-dihydroquinolin-2(1)-one derivatives in high yields. Moreover, this method could be utilized in the late-stage modifications of bioactive molecules.
已开发出一种铜/钯催化的炔基连接的α-溴代羰基化合物与酚类的串联自由基环化和羰基化反应，用于快速构建含酯的3,4-二氢喹啉-2(1)-酮骨架。通过使用苯-1,3,5-三基三甲酸酯（TFBen）作为一氧化碳源，反应顺利进行，以高产率得到了一系列含酯的3,4-二氢喹啉-2(1)-酮衍生物。此外，该方法可用于生物活性分子的后期修饰。
