14906-61-7Relevant academic research and scientific papers
One step conversion of heteroaromatic-N-oxides to imidazolo-heteroarenes
Keith, John M.
, p. 327 - 330 (2008)
(Chemical Equation Presented) Various pyridine-, quinoline-, isoquinoline-, and pyrimidine-N-oxides were converted to their corresponding α-imidazoloheteroarenes in good yield by treatment with sulfuryl diimidazole in nonpolar solvents at elevated tempera
Heterocyclic compound used as MNK inhibitor
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Paragraph 0262, (2019/01/08)
The invention relates to a heterocyclic compound, a pharmaceutical composition containing the heterocyclic compound, a preparation method thereof, and application thereof used as a mitogen activated protein kinase interacting kinase 1 and 2-MNK1/MNK2 inhibitor. The inhibitor is the heterocyclic compound as shown in the formula (I), or its pharmaceutically acceptable salt, prodrug, solvent compound, polycrystal, isomer, stable isotope derivative or a pharmaceutical composition containing the heterocyclic compound. The compound of the invention can be used for treating or preventing MNK-mediatedrelated diseases, such as cancers.
Synthesis method of heterocyclic compound 3-methoxypyridine
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, (2017/08/17)
The invention discloses a synthesis method of a heterocyclic compound 3-methoxypyridine. The method comprises the following steps: putting raw materials, i.e., 3-halogenated pyridine, hydrogen peroxide and acetic acid into a three-mouth flask, carrying out reaction for 4-8h at the temperature of 40-80 DEG C under the condition of stirring, recovering the acetic acid, adding a saturated sodium carbonate solution and stirring to enable a system to be alkaline, evaporating to remove water, then adding chloroform for washing, and carrying out vacuum distillation to obtain N-oxide-3-halogenated pyridine; respectively adding the N-oxide-3-halogenated pyridine, metal salt of alkyl alcohol, a catalyst A and alcohol into the three-mouth flask, carrying out reflux reaction for 5-8h under the condition of stirring, then cooling, neutralizing a product to be neutral, and carrying out distillation to obtain N-oxide-3-alkyloxypyridine; respectively adding the N-oxide-3-alkyloxypyridine, ferric trichloride, hydrazine hydrate, activated carbon and ethanol into the three-mouth flask, carrying out reaction at the temperature of 70 DEG C for 3h, cooling to room temperature, and carrying out vacuum distillation to obtain the 3-methoxypyridine. The synthesis method is high in intermediate conversion rate, mild in reaction conditions, safe in operation, low in price of raw materials and easy in raw material obtaining, thus being suitable for industrial production.
Solvent- and halide-free synthesis of pyridine-2-yl substituted ureas through facile C-H functionalization of pyridine: N -oxides
Rassadin, Valentin A.,Zimin, Dmitry P.,Raskil'dina, Gulnara Z.,Ivanov, Alexander Yu.,Boyarskiy, Vadim P.,Zlotskii, Semen S.,Kukushkin, Vadim Yu.
supporting information, p. 6630 - 6636 (2018/03/01)
A novel solvent- and halide-free atom-economical synthesis of practically useful pyridine-2-yl substituted ureas utilizes easily accessible or commercially available pyridine N-oxides (PyO) and dialkylcyanamides. The observed C-H functionalization of PyO is suitable for the good-to-high yielding synthesis of a wide range of pyridine-2-yl substituted ureas featuring electron donating and electron withdrawing, sensitive, or even fugitive functional groups at any position of the pyridine ring (63-92%; 19 examples). In the cases of 3-substituted PyO, the C-H functionalization occurs regioselectively providing a route for facile generation of ureas bearing a 5-substituted pyridine-2-yl moiety.
SMALL MOLECULE AGONISTS OF NEUROTENSIN RECEPTOR 1
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Paragraph 00659, (2016/04/26)
Provided herein are small molecule neurotensin receptor agonists, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.
Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
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, (2008/06/13)
Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.
A simple and efficient method for the preparation of N- heteroaromatic N-oxides
Balicki, Roman,Golinski, Jerzy
, p. 1529 - 1534 (2007/10/03)
Urea-hydrogen peroxide/formic acid system has shown utility for mild and safe N-oxidation of N-heteroaromatic compounds.
Deoxydative Thiation of 3-Substituted Pyridine N-Oxides with 4-Methoxytoluene-α-thiol: A Divergent Route to Pyridinethiols
Sato, Nobuhiro,Nagano, Eiichi
, p. 691 - 698 (2007/10/02)
Synthesis of 3-substituted 2-pyridinethiols was achieved by thiation of pyridine N-oxides with 4-methoxytoluene-α-thiol in the presence of diethylcarbamoyl chloride followed by cleavage of the resulting sulfides.The case of substitution was shown to be affected by nucleophilicity of the N-oxide oxygen.Addition of zinc bromide to the reaction, a need for triethylamine, decreased most of the yield for thiation products but the formation of 3-methoxy-2-methoxybenzylthiopyridine was only improved.A plausible mechanism of the substitution, particularly β-thiation to the N-oxide function, is discussed compared with the regiochemistry observed in the reaction with diethoxyphosphoryl chloride instead of diethylcarbamoyl chloride.The debenzylation to pyridinethiol was also found to be dependent on the electron-density in the pyridine ring.
Spectroscopic Study of Hydrophobic Interaction of Heterocyclic Amine N-Oxides with Cyclodextrins
Uno, Bunji,Kaida, Naoki,Kawakita, Toshio,Kano, Kenji,Kubota, Tanekazu
, p. 3753 - 3759 (2007/10/02)
Electronic spectra of aromatic amine N-oxides show a marked blue shift with the change of solvent polarity from aprotic solvents to protic ones.This is very useful to examine the hydrophobic interaction between the amine N-oxides and cyclodextrins (CyD) in water.Among the various systems studied a typical example is the system of 4-nitroquinoline N-oxide (4NQO) and 2,6-di-O-methyl-β-cyclodextrin in water.A clear red shift of the ultraviolet (UV) spectrum of 4NQO was observed upon inclusion complex formation, indicating directly that the CyD cage environment is much more hydrophobic than in water.Thermodynamic and spectroscopic constants pertinent to those inclusion complex formations were evaluated and the results are discussed in relation to the complex formation mechanisms.
