142057-77-0Relevant articles and documents
Fractal analysis of catalyst surface morphologies on hydrogenation in process of 2-((1-benzylpiperidin-4-yl)methyl)-5,6-dimethoxy-2,3-dihydroinden-1- one hydrochloride synthesis
Jel?i?, ?elimir,Samard?i?, Zrinka Masteli?,Zrn?evi?, Stanka
, p. 30 - 43 (2013)
Catalytic hydrogenation of 2-((1-benzyl-1,2,3,6-tetrahydropyridin-4-yl) methylene)-5,6-dimethoxy-2,3-dihydroinden-1-one hydrochloride (1) to 2-((1-benzylpiperidin-4-yl)methyl)-5,6-dimethoxy-2,3-dihydroinden-1-one hydrochloride (2) was investigated in batch-slurry reactor. The 5% Pt/C catalysts were chosen for optimizing the catalytic activity. The catalyst activity has been changed by using the differently morphologically structured fractal catalysts. The kinetic terms of hydrogenation for (1) change with the fractal dimensions of the 5% Pt/C catalyst. The most active and selective (with the highest reaction rate for production of (2), and with the least impurities level) is the catalyst K3, and the worst the catalyst K4. This most active and selective catalyst has an intermediate fractal surface dimension, D F,ads = 2.77, and the worst catalyst is represented by almost smooth surface with a high DF,ads = 2.82. The interface D[BW] fractal indices (derived from the thresholded SEM images, at the magnifications in the range 600-2000×) are largest ones for the most suitable catalyst K3, and lowest for the catalyst K4.
Can Heteroarenes/Arenes Be Hydrogenated Over Catalytic Pd/C Under Ambient Conditions?
Tanaka, Nao,Usuki, Toyonobu
, p. 5514 - 5522 (2020/07/24)
Hydrogenation of over a dozen aromatic compounds, including both heteroarenes and arenes, over palladium on carbon (Pd/C, 1–100 molpercent) with H2-balloon pressure at room temperature is reported. Analyses using pyridine as a model substrate revealed that acetic acid was the best solvent, as using only 1 molpercent Pd/C provided piperidine quantitatively. Substrate scope analysis and density functional theory calculations indicated that reaction rates are highly dependent on frontier molecular orbital characteristics and the steric bulkiness of substituents. Moreover, the established method was used for the concise synthesis of the anti-Alzheimer drug donepezil (Aricept?).
Purification method for Donepezil
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Paragraph 0031, (2019/12/25)
The invention relates to a purification method for Donepezil and belongs to the technical field of preparation of raw pharmaceutical materials. The purification method for the Donepezil or pharmaceutically acceptable salts thereof, provided by the invention, comprises the steps: firstly, adding a hydrophobic organic solvent and water into the Donepezil or pharmaceutically acceptable salts thereof,so as to obtain a mixed solution, wherein the hydrophobic organic solvent is selected from dichloromethane, ethyl acetate, toluene and mixtures thereof; adjusting an aqueous phase pH of the mixed solution to be not smaller than 9 with alkali, and separating an organic phase from an aqueous phase; and subjecting the organic phase obtained in the step (3) to depressurized concentration, thereby obtaining purified Donepezil. According to the purification method for the Donepezil or pharmaceutically acceptable salts thereof, provided by the invention, high-quality raw pharmaceutical materials areprovided for preparations.