24619-86-1Relevant academic research and scientific papers
Simplified preparation of a graphene-co-shelled Ni/NiO@C nano-catalyst and its application in theN-dimethylation synthesis of amines under mild conditions
Liu, Jianguo,Ma, Longlong,Song, Yanpei,Zhang, Mingyue,Zhuang, Xiuzheng
supporting information, p. 4604 - 4617 (2021/06/30)
The development of Earth-abundant, reusable and non-toxic heterogeneous catalysts to be applied in the pharmaceutical industry for bio-active relevant compound synthesis remains an important goal of general chemical research.N-methylated compounds, as one of the most essential bioactive compounds, have been widely used in the fine and bulk chemical industries for the production of high-value chemicals. Herein, an environmentally friendly and simplified method for the preparation of graphene encapsulated Ni/NiO nanoalloy catalysts (Ni/NiO@C) was developed for the first time, for the highly selective synthesis ofN-methylated compounds using various functional amines and aldehydes under easy to handle, and industrially applicable conditions. A large number of primary and secondary amines (more than 70 examples) could be converted to the correspondingN,N-dimethylamines with the participation of different functional aldehydes, with an average yield of over 95%. A gram-scale synthesis also demonstrated a similar yield when compared with the benchmark test. In addition, it was further proved that the catalyst could easily be recycled because of its intrinsic magnetism and reused up to 10 times without losing its activity and selectivity. Also, for the first time, the tandem synthesis ofN,N-dimethylamine products in a one-pot process, using only a single earth-abundant metal catalyst, whose activity and selectivity were more than 99% and 94%, respectively, for all tested substrates, was developed. Overall, the advantages of this newly developed method include operational simplicity, high stability, easy recyclability, cost-effectiveness of the catalyst, and good functional group compatibility for the synthesis ofN-methylation products as well as the industrially applicable tandem synthesis process.
Design, synthesis and evaluation of tacrine based acetylcholinesterase inhibitors
Shen, Yanhong,Yu, Youzhu,Lv, Huichao,Feng, Liping,Zhang, Guoqiang
scheme or table, p. 341 - 345 (2011/10/18)
A series of tacrine based cholinesterase inhibitors was designed, synthesized and assayed for their biological activity. Among them, five compounds inhibited acetylcholinesterase in micromolar range and most of the compounds demonstrated much better selectivity for AChE than reference compound tacrine.
Design, synthesis and evaluation of galanthamine derivatives as acetylcholinesterase inhibitors
Jia, Ping,Sheng, Rong,Zhang, Jing,Fang, Liang,He, Qiaojun,Yang, Bo,Hu, Yongzhou
experimental part, p. 772 - 784 (2009/09/05)
A new series of galanthamine derivatives have been designed, synthesized and evaluated as acetylcholinesterase inhibitors. All of the new compounds prepared showed high AChE inhibitory activities, with compound 3e that has an N-hexyl-benzyl piperidine substituent on the nitrogen atom reaching the best inhibitory activity for AChE (IC50 = 5.62 nM). The docking study performed with AutoDock demonstrated that 3e was nicely accommodated by AChE.
Synthesis and antimalarial activity of new analogues of amodiaquine
Delarue-Cochin, Sandrine,Paunescu, Emilia,Maes, Louis,Mouray, Elisabeth,Sergheraert, Christian,Grellier, Philippe,Melnyk, Patricia
, p. 252 - 260 (2008/09/18)
In order to determine the real significance of the 4′-phenolic group in the antimalarial activity and/or cytotoxicity of amodiaquine (AQ), analogues for which this functionality was shifted or modified were synthesized. Good in vitro antimalarial activity
Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors
Sheng, Rong,Lin, Xiao,Li, Jingya,Jiang, Yanke,Shang, Zhicai,Hu, Yongzhou
, p. 3834 - 3837 (2007/10/03)
A series of 2-phenoxy-indan-1-one derivatives have been designed, synthesized, and tested as acetylcholinesterase inhibitors. The most potent compound exhibited high AChE inhibitory activity (IC50 = 50 nM), and the molecular docking study indicated that it was nicely accommodated by AChE.
REACTIVITY OF NEW PRECURSORS OF QUINONE METHIDES
Loubinoux, Bernard,Miazimbakana, Joseph,Gerardin, Philippe
, p. 1939 - 1942 (2007/10/02)
The azidomethylene protecting group allows the synthesis of unstable phenolic compounds which are used as quinone methide precursors in the alkylations of alcohols, phenols, azide, thiophenol, amines, enols and enolates.
