With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1254058-34-8,3-Methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)aniline,as a common compound, the synthetic route is as follows.
(5) Under an argon atmosphere, to a mixture of 2-chloro-5-[(2,6-difluoro-3,5-dimethoxybenzyl)oxy]pyrimidine (1.03 g), 3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]aniline (1.29 g), 1,1′-binaphthalene-2,2′-diylbis(diphenylphosphine) (609 mg), cesium carbonate (3.19 g), and dioxane (20.6 mL) was added palladium acetate (146 mg) at room temperature, followed by stirring at 100 C. for 4 hours. To the reaction mixture was added water, followed by extraction with ethyl acetate. The organic layer was washed with saturated brine, dried over anhydrous magnesium sulfate, and then filtered. The filtrate was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (chloroform/methanol/concentrated aqueous ammonia), purified by basic silica gel columnchromatography (ethyl acetate), and then solidified with ethyl acetate and then with ethanol to obtain 5-[(2,6-difluoro-3,5-dimethoxybenzyl)oxy]-N-{3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}pyrimidin-2-amine (Compound A: 830 mg). MS (ESI+): 585 [(M+H)+]. NMR (DMSO-d6): 1.45-1.60 (2H, m), 1.73-1.84 (2H, m), 2.14 (3H, s), 2.17-2.58 (11H, m), 3.24-3.36 (2H, m), 3.75 (3H, s), 3.87 (6H, s), 5.16 (2H, s), 6.79 (1H, d, J=8.8 Hz), 7.07 (1H, t, J=8.4 Hz), 7.24 (1H, dd, J=8.8, 2.4 Hz), 7.32 (1H, d, J=2.4 Hz), 8.29 (2H, s), 9.21 (1H, s)., 1254058-34-8
1254058-34-8 3-Methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)aniline 68014035, apiperidines compound, is more and more widely used in various fields.
Reference£º
Patent; ASTELLAS PHARMA INC.; FUTAMI, Takashi; TAKESHITA, Rumi; (12 pag.)US2016/199371; (2016); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem