5961-59-1Relevant articles and documents
N-Methylation of p-Anisidine on the Catalysts Based on Cu-Containing Layered Double Hydroxides
Bukhtiyarova,Nuzhdin,Kardash, T. Yu.,Bukhtiyarov,Gerasimov, E. Yu.,Romanenko
, p. 343 - 354 (2019)
Abstract: Cu-containing layered double hydroxides with different Cu : Al ratios are synthesized by co-precipitation using a mixture of hydroxide and sodium carbonate as a precipitation agent. The influence of the precipitation agent concentration on the formation of the hydrotalcite phase was studied by thermal analysis and X-ray diffraction. The surface of the obtained samples after calcination at 450°C and their subsequent reduction at 300°C in hydrogen, was characterized by X-ray photoelectron spectroscopy and transmission electron microscopy. The synthesized catalysts were tested in the reaction of N-methylation of p-anisidine with methanol in an autoclave reactor to produce N-methyl-p-anisidine. The influence of the Cu : Al ratio in them on the catalytic activity and selectivity was studied.
AQ-4, a deuterium-containing molecule, acts as a microtubule-targeting agent for cancer treatment
Chen, Hua-Lin,Gong, Sha,Hu, Ya-Guang,Huang, Hui,Lin, Bi-Yun,Liu, Wen-Lin,Lu, Yuan-Zhi,Meng, Yu-Hua,Yan, Jun
, (2020)
The important physiological function of microtubules makes them an indispensable and clinically effective target of anti-tumor agents. Herein, we sought to design, synthesize, and evaluate a novel 4-anilinoquinazoline derivative and identify its anti-tumor activity in vitro and in vivo. The novel compound, N-(4-methoxyphenyl)-N-methyl-2-(methyl-d3)quinazolin-4-amine (AQ-4), was identified as a representative scaffold and potent microtubule-targeting agent. As a promising antimitotic agent, AQ-4 displayed remarkable anti-tumor activity with an average IC50 value of 19 nM across a panel of 14 human cancer cell lines. AQ-4 also exhibited nearly identical potent activities against drug-resistant cells, with no evidence of toxicity towards normal cells. A further target verification study revealed that AQ-4 targets the tubulin-microtubule system by significantly inhibiting tubulin polymerization and disrupting the intracellular microtubule spindle dynamics. According to the results of mechanism study, AQ-4 induced cell cycle arrest in the G2/M phase, promoting evident apoptosis and a collapses of mitochondrial membrane potential. The superior anti-tumor effect of AQ-4 in vivo suggests that it should be further investigated to validate its use for cancer therapy.
Photoinduced Hydroarylation and Cyclization of Alkenes with Luminescent Platinum(II) Complexes
Cheng, Hanchao,Lam, Tsz-Lung,Liu, Yungen,Tang, Zhou,Che, Chi-Ming
supporting information, p. 1383 - 1389 (2020/11/30)
Photoinduced hydroarylation of alkenes is an appealing synthetic strategy for arene functionalization. Herein, we demonstrated that aryl radicals generated from electron-deficient aryl chlorides/bromides could be trapped by an array of terminal/internal aryl alkenes in the presence of [Pt(O^N^C^N)] under visible-light (410 nm) irradiation, affording anti-Markovnikov hydroarylated compounds in up to 95 % yield. Besides, a protocol for [Pt(O^N^C^N)]-catalyzed intramolecular photocyclization of acrylanilides to give structurally diverse 3,4-dihydroquinolinones has been developed.
Method for realizing N-alkylation by using alcohols as carbon source under photocatalysis
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Paragraph 0048-0057, (2021/03/13)
The invention discloses a method for realizing N-alkylation by using alcohols as a carbon source under photocatalysis, and belongs to the technical field of catalytic synthesis. Alcohol, a substrate raw material and a catalyst are placed in a reaction device, ultraviolet and/or visible light irradiation is carried out in an inert atmosphere, after the irradiation is finished, solid-liquid separation is carried out to remove the catalyst, and an N-alkylation product can be obtained through extraction, distillation and purification, wherein the substrate raw material comprises any one of an amine compound, an aromatic nitro compound or an aromatic nitrile compound, the alcohol comprises any one or more of soluble primary alcohols, and the catalyst is metal oxide/titanium dioxide or metal sulfide/titanium dioxide. The method is simple and easy to operate, can be used for efficient photocatalysis one-pot multi-step hydrogenation N-alkylation reaction, and is mild in reaction condition, high in chemical selectivity of N-alkylamine, good in catalyst stability and easy to recycle.