1354833-83-2Relevant academic research and scientific papers
Development of a copper(II)-catalyzed three-component tandem synthesis of isoindolinone derivatives
Sun, Leon Xuetong,Zeng, Tieqiang,Jiang, Dong,Dai, Li-Yi,Li, Chao-Jun
experimental part, p. 92 - 99 (2012/03/07)
Isoindolinone derivatives are important pharmaceutical building blocks in medicinal chemistry. Isoindolo[2,1-a]quinolines are a class of interesting compounds that possess protective effects against N2-induced hypoxia and inhibitory activities against human topoisomerase II and bacterial DNA-gyrase. The conventional methods for synthesizing these compounds are unsatisfactory because of their harsh reaction conditions, complex starting materials, and multistaged purification procedures. This synthesis of the propargyl-isoindolinone core features an aldehyde-alkyne-amine (A3) coupling-based tandem strategy using methyl 2-formylbenzoate, primary aryl amine, and terminal alkyne under Cu(OTf)2 catalysis.
