7259-53-2Relevant academic research and scientific papers
Ozone-Mediated Amine Oxidation and Beyond: A Solvent-Free, Flow-Chemistry Approach
Skrotzki, Eric A.,Vandavasi, Jaya Kishore,Newman, Stephen G.
, p. 14169 - 14176 (2021/06/30)
Ozone is a powerful oxidant, most commonly used for oxidation of alkenes to carbonyls. The synthetic utility of other ozone-mediated reactions is hindered by its high reactivity and propensity to overoxidize organic molecules, including most solvents. This challenge can largely be mitigated by adsorbing both substrate and ozone onto silica gel, providing a solvent-free oxidation method. In this manuscript, a flow-based packed bed reactor approach is described that provides exceptional control of reaction temperature and time to achieve improved control and chemoselectivity over this challenging transformation. A powerful method to oxidize primary amines into nitroalkanes is achieved. Examples of pyridine, C-H bond, and arene oxidations are also demonstrated, confirming the system is generalizable to diverse ozone-mediated processes.
The M?CPbA?NH3(G) system: A safe and scalable alternative for the manufacture of (substituted) pyridine and quinoline N?oxides?
Palav, Amey,Misal, Balu,Ernolla, Anilkumar,Parab, Vinod,Waske, Prashant,Khandekar, Dileep,Chaudhary, Vinay,Chaturbhuj, Ganesh
supporting information, p. 244 - 251 (2019/03/17)
An improved, safe, and scalable isolation process for (substituted) pyridine and quinoline N-oxides in quantitative yields along with high purities using the m-CPBA?NH3(g) system is described. The safety was assessed by reaction calorimetry and differential scanning calorimetry studies for possible hazards during the conversion and isolation steps. Careful interpretation of the data substantiated the safety and scalability. The process flow is simplified to meet the industrial requirements of safety, cost-effectiveness, and utility minimization. The reaction was safely demonstrated at a 2.5 kg scale.
URIDINE NUCLEOSIDE DERIVATIVES, COMPOSITIONS AND METHODS OF USE
-
Paragraph 0211, (2018/04/20)
This disclosure relates to uridine nucleoside derivatives, compositions comprising therapeutically effective amounts of those nucleoside derivatives and methods of using those nucleoside derivatives or compositions in treating disorders that are responsive to compounds, such as agonists, of P2Y6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease, Parkinson's disease) and traumatic CNS injury, pain, Down Syndrome (DS), glaucoma and inflammatory conditions.
Synthesis and crystal structure of an M4L6 tetrahedral cage with outward-facing pockets from a substituted pyrazolyl-pyridine ligand
Rasbia, Nawal K. Al,Ward, Michael D.
, p. 961 - 966 (2018/08/17)
The self-assembly of metal-polydentate ligands to give supramolecular tetrahedral complexes is of considerable current interest. A new ligand, 4-benzyl- 2-[1-(2-{[3-(4-benzylpyridin-2-yl)-1H-pyrazol-1-yl]methyl}benzyl)-1H-pyrazol- 3-yl]pyridine (L), with
Nickel-catalyzed C–H trifluoromethylation of pyridine N-oxides with Togni's reagent
Gao, Xianying,Geng, Yang,Han, Shuaijun,Liang, Apeng,Li, Jingya,Zou, Dapeng,Wu, Yangjie,Wu, Yusheng
supporting information, p. 1551 - 1554 (2018/03/23)
The first nickel-catalyzed C–H trifluoromethylation of pyridine N-oxides with Togni's reagent has been achieved. Trifluoromethylation proceeds smoothly under mild conditions with moderate functional group compatibility. Notable advantages of this method include the using of low cost of nickel catalyst, and its simple convenient operation.
Aza-and polyaza-naphthalenly ketones useful as hiv integrase inhibitors
-
Page/Page column 46; 60, (2010/02/10)
Certain aza- and polyaza-naphthalenyl ketones including certain quinolinyl and naphthyridinyl ketones are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment or the delay in the onset of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells
Zhuang, Linghang,Wai, John S.,Embrey, Mark W.,Fisher, Thorsten E.,Egbertson, Melissa S.,Payne, Linda S.,Guare Jr., James P.,Vacca, Joseph P.,Hazuda, Daria J.,Felock, Peter J.,Wolfe, Abigail L.,Stillmock, Kara A.,Witmer, Marc V.,Moyer, Gregory,Schleif, William A.,Gabryelski, Lori J.,Leonard, Yvonne M.,Lynch Jr., Joseph J.,Michelson, Stuart R.,Young, Steven D.
, p. 453 - 456 (2007/10/03)
Naphthyridine 7 inhibits the strand transfer of the integration process catalyzed by integrase with an IC50 of 10 nM and inhibits 95% of the spread of HIV-1 infection in cell culture at 0.39 μM. It does not exhibit cytotoxicity in cell culture
Subtype-selective NMDA receptor ligands and the use thereof
-
, (2008/06/13)
The invention relates to subtype-selective NMDA receptor ligands and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neuro-degenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the overstimulation of the excitatory amino acids, treating anxiety, psychosis, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headache, chronic pain, Parkinson's disease, glaucoma, CMV retinitis, urinary incontinence, opioid tolerance or withdrawal, and inducing anesthesia, as well as for enhancing cognition.
Evaluation of the Polar-Inductive and Mesomeric Effects exerted on Contiguous Functionalities by N-Oxidopyridinium Groups
Barchiesi, Emma,Bradamante, Silvia,Carfagna, Carla,Ferraccioli, Raffaella,Giorgio, A.,Pagni, Giorgio A.
, p. 1009 - 1014 (2007/10/02)
The polar-inductive and mesomeric effects (and mixtures thereof) of N-oxipyridinium-2-, -3-, and 4-yl functionalities have been evaluated in terms of the δIB, δR-, and δ-C scales previously defined.Values were generated fr
Bridged-ring Nitrogen Compounds. Part 5. Synthesis of 2,6-Methano-3-benzazonine ring-system
Proctor, George R.,Smith, Francis J.
, p. 1754 - 1762 (2007/10/02)
Syntheses of cis- and trans-4-benzyl- and 4-(3-methoxybenzyl)-2-methoxycarbonyl-1-methylpiperidines are described; amino-acids and amino-alcohols obtained from these compounds failed to cyclise. cis-2-Benzyl-4-ethoxycarbonyl-1-methylpiperidine has been ma
