365213-40-7Relevant academic research and scientific papers
Preparation method of imidazole [1, 2-a] pyridine-containing secondary amine and tertiary amine derivatives
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Paragraph 0096-0104, (2021/09/04)
The invention provides a preparation method of imidazo [1, 2-a] pyridine-containing secondary amine and tertiary amine derivatives from triazine compounds and imidazo [1, 2-a] pyridine, and relates to the field of medicinal chemistry. According to the present invention, the triazine compound is reacted with the imidazo [1, 2-a] pyridine compound, the Lewis acid catalysis is performed, the reaction conditions such as the reaction temperature and the reaction time are controlled, and the controllable cracking and the fixed-point selectivity of the triazine compound are utilized to synthesize different imidazo [1, 2-a] pyridine-containing secondary amine and tertiary amine derivatives, such that the synthesis method is simple, the multi-step reaction is not required, the product purity and yield are high, selectable substrate range is wide, and the preparation method can be well applied to the field of pharmacy.
Aminomethylation of imidazopyridines using N,N-dimethylformamide as an aminomethylating reagent under Cu(II)-catalysis
Ghosh, Payel,Samanta, Sadhanendu,Ghosh, Sumit,Jana, Sourav,Hajra, Alakananda
supporting information, (2020/11/10)
N,N-Dimethylformamide has been explored as an aminomethylating reagent in the functionalization of imidazopyridine under Cu(II)-catalysis. A library of aminomethylated imidazopyridines with broad functionalities was synthesized in good yields.
A structure-activity relationship study of the affinity of selected imidazo[1,2-a]pyridine derivatives, congeners of zolpidem, for the ω1-subtype of the benzodiazepine receptor
Lange,Karolak-Wojciechowska,Wejroch,Rump
, p. 43 - 52 (2007/10/03)
A series of 6-substituted 2-aryl-N,N-dimethylimidazol [1,2-a]pyridine-3-acetamides, congeners of zolpidem and alpidem, was synthesized and tested in vitro for binding with the benzodiazepine receptor in the competition with 3H-zolpidem as an ω1-selective radioligand. Molecular electrostatic potential (MEP) and the HOMO and LUMO energies were calculated for the compounds by semi-empirical quantum chemistry methods. The lipophilicity parameter of the compounds, expressed as the logarithm of the octanol-water partition coefficient (log P), was calculated; alternatively, standard values of the Hansch hydrophobic substituent constants π were used. In agreement with earlier investigations on the benzodiazepine receptor ligands with a high preference for the ω1-subtype, a quantitative correlation of the biological data with molecular parameters has revealed a significant dependence (r=0.954) of the binding affinity (IC50) on the deepest MEP minimum, in this case associated with the amide carbonyl oxygen atom. The lipophilicity parameters were found to be of lower significance.
