In this article, an effective feasible method to synthesize translocator protein 18kDa （TSPO） imidazopyridine ligand 7 is discussed. A new procedure for the synthesis of the key intermediate 17 has been developed in...In this article, an effective feasible method to synthesize translocator protein 18kDa （TSPO） imidazopyridine ligand 7 is discussed. A new procedure for the synthesis of the key intermediate 17 has been developed in four steps （condensation, diazo reaction, hydrolysis, amidation） from 2-aminopyridine 18. The overall yield was increased from 18% to 31.6%. One of the key steps is using activated copper powder as a catalyst in several cycles. Finally, reduction of 17 with Zn dust completed the synthesis of TSPO imidazopyridine ligand 7 in 86% yield.展开更多
基金Supported by the National Natural Science Foundation of China(81373254,81373254,81071182)the Applied Basic Research Program of Wuhan Municipal Bureau of Science and Technology(2013020501010176)+3 种基金the Scientific and Technological Innovative Research Team of Wuhan(2013070204020048)Academic Award for Excellent Ph.D. Candidates Funded by Ministry of Education of China(5052012306001)Innovation Seed Fund of Wuhan University School of Medicine,the Fundamental Research Funds for the Central Universities(2012306020201)Medical Innovation Foundation of Fujian Province,China(2009-CXB-46)
文摘In this article, an effective feasible method to synthesize translocator protein 18kDa （TSPO） imidazopyridine ligand 7 is discussed. A new procedure for the synthesis of the key intermediate 17 has been developed in four steps （condensation, diazo reaction, hydrolysis, amidation） from 2-aminopyridine 18. The overall yield was increased from 18% to 31.6%. One of the key steps is using activated copper powder as a catalyst in several cycles. Finally, reduction of 17 with Zn dust completed the synthesis of TSPO imidazopyridine ligand 7 in 86% yield.
