An efficient method for the synthesis of [1,2,3]triazolo[1,5-a]quinoxalin-4(5H)-ones and 1H-[1,2,3]triazolo[4,5-c]quinolin-4(5H)-ones

Drs. CAI Qian and DING Ke Dings’ research teams at GIBH recently developed an efficient method　for　the synthesis of [1,2,3]triazolo[1,5-a]quinoxalin-4(5H)-ones and 1H-[1,2,3]triazolo[4,5-c]quinolin-4(5H)-ones through a novel copper-catalyzed  tandem reaction by utilizing two famous copper-catalyzed reactions, CuAAC and Ullmann coupling. The trapping of the C-Cu intermediate produced in CuAAC led to further formation of an aryl C-C bond through intramolecular Ullmann C-C coupling.

This method of synthesis can offer a simple and more efficient pathway for drug discoveries and other related research.This work has been published in Org.Lett. 2012, 14, 1262-1265 (http://pubs.acs.org/doi/abs/10.1021/ol300114w?prevSearch=jiajie%2Byan&searchHistoryKey=) and Org.Lett. 2012,14 3332-3335(http://pubs.acs.org/doi/abs/10.1021/ol301307x?prevSearch=jiajie%2Byan&searchHistoryKey=). This project was funded by National Science Foundation of China (21002102)National Major Scientific and Technological Special Project for “Significant New Drugs Development”（2011ZX09102-010）and “Hundred Talent Project” of the Chinese Academy of Science.

The synthesis of [1,2,3]triazolo[1,5-a]quinoxalin-4(5H)-ones and 1H-[1,2,3]triazolo[4,5-c]quinolin-4(5H)-ones