A Practical Process for the Synthesis of Translocator Protein 18kDa Imidazopyridine Ligand  

作　　者：WEN Meng QU Chunrong SU Xinhui DING Mingmin DENG Zixin HONG Xuechuan 

机构地区：[1]Key Laboratory of Combinatorial Biosynthesis and Drug Discovery of Ministry of Education/School of Pharmaceutical Sciences, Wuhan University [2]Department of Nuclear Medicine and Minnan PET Center, the First Affiliated Hospital, Xiamen University

出　　处：《Wuhan University Journal of Natural Sciences》2014年第1期19-26,共8页武汉大学学报（自然科学英文版）

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);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)

摘　　要：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.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.

关 键 词：translocatorprotein 18kDa （TSPO） synthesis IMIDAZOPYRIDINE activated copper ANTITUMOR 

分 类 号：O62[理学—有机化学]