An efficient acetic acid mediated metal-free oxidative C—H cross coupling of imidazo[1,2-a]pyridines with glyoxal hydrates has been developed under air atmosphere.The present protocol exhibits broad substrate scope,g...An efficient acetic acid mediated metal-free oxidative C—H cross coupling of imidazo[1,2-a]pyridines with glyoxal hydrates has been developed under air atmosphere.The present protocol exhibits broad substrate scope,good functional group tolerance,and enables the construction of a series of 1,2-dicarbonyl imidazo[1,2-a]pyridines in good yields.The reaction mechanism studies suggest that the reactions proceed through the electrophilic substitution and subsequent oxidation pathway.展开更多
The first successful lithium bromide mediated solvent free condensation of arylenediamine and esters to obtain 2-substituted benzimidazole and imidazopyridine in good to excellent yields is described.
The visible light promoted C-H sulfonylmethylation of imidazopyridines with easily accessible bromomethyl sulfones under mild reaction conditions was described.This protocol provides an effective and practical access ...The visible light promoted C-H sulfonylmethylation of imidazopyridines with easily accessible bromomethyl sulfones under mild reaction conditions was described.This protocol provides an effective and practical access to sulfonylmethylated imidazopyridines with good functional group tolerance.The desired products were provided in moderate to excellent yields for 50 examples at room temperature.The method could also be an attractive strategy to install a methyl group on imidazopyridines.展开更多
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
文摘An efficient acetic acid mediated metal-free oxidative C—H cross coupling of imidazo[1,2-a]pyridines with glyoxal hydrates has been developed under air atmosphere.The present protocol exhibits broad substrate scope,good functional group tolerance,and enables the construction of a series of 1,2-dicarbonyl imidazo[1,2-a]pyridines in good yields.The reaction mechanism studies suggest that the reactions proceed through the electrophilic substitution and subsequent oxidation pathway.
文摘The first successful lithium bromide mediated solvent free condensation of arylenediamine and esters to obtain 2-substituted benzimidazole and imidazopyridine in good to excellent yields is described.
基金financially supported by the National Natural Science Foundation of China (No.21602046)the MOST of China (No.2016YFE0132600)the Doctor’s Scientific Research Foundation of Henan University of Chinese Medicine (No.BSJJ2016-12)
文摘The visible light promoted C-H sulfonylmethylation of imidazopyridines with easily accessible bromomethyl sulfones under mild reaction conditions was described.This protocol provides an effective and practical access to sulfonylmethylated imidazopyridines with good functional group tolerance.The desired products were provided in moderate to excellent yields for 50 examples at room temperature.The method could also be an attractive strategy to install a methyl group on imidazopyridines.
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.
