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
The normal development and optimal functioning of the brain requires a vigilant immune surveillance system to detect and remove potential risk factors and prevent infection and tissue damage. Microglia are the residen...The normal development and optimal functioning of the brain requires a vigilant immune surveillance system to detect and remove potential risk factors and prevent infection and tissue damage. Microglia are the resident immune cells and the frontline defenders responsible for the immune response of the brain. Resting microglia possess a ramified morphology with numerous thin processes that continuously sample the environment. In response to inflammatory signals, microglia become activated and transform their morphology into a thick, amoeboid-like shape. Activated microglia proliferate, tolerate to sites of iniurv,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.
基金supported by the Bio&Medical Technology Development Program of the National Research Foundation of Korea(NRF)grant(No.2012M3A9C6049935)the DGIST Convergence Science Center Program(15-BD-04)of the Ministry of Science,ICT and Future Planning of Korea
文摘The normal development and optimal functioning of the brain requires a vigilant immune surveillance system to detect and remove potential risk factors and prevent infection and tissue damage. Microglia are the resident immune cells and the frontline defenders responsible for the immune response of the brain. Resting microglia possess a ramified morphology with numerous thin processes that continuously sample the environment. In response to inflammatory signals, microglia become activated and transform their morphology into a thick, amoeboid-like shape. Activated microglia proliferate, tolerate to sites of iniurv,
