Day: October 14, 2022

SDS of cas: 128071-75-0In 2020 ,《Synthetic Strategy Studies for a Concise Access to Functionalized Pyrano[4,3-b]pyridin-7-ones: An Entry to Semi-Rigid Analogs of Antihistamines》 appeared in European Journal of Organic Chemistry. The author of the article were Beghennou, Anissa; Passador, Kevin; Passador, Anthony; Corce, Vincent; Thorimbert, Serge; Botuha, Candice. The article conveys some information:

We report short and efficient syntheses of polyfunctionalized 5,8-dihydro-7H-pyrano[4,3-b]pyridin-7-ones and 1,4-dihydro-3H-pyrano[4,3-c]pyridin-3-ones which can be considered as new aza analogs of 3-isochromanones and as promising scaffolds for medicinal chem. Depending on the nature of the substituent, three different and complementary synthetic methodologies were used allowing the introduction of significant diversity in the substituent on the lactone ring of the pyranopyridinones. The selective α-arylation of nitrile (SNAr) and tert-Bu ester enolate (Pd catalyzed) followed by an acidic mediated lactonization gives access to original C8-functionalized pyrano[4,3-b]pyridin-7-ones and a seleno-mediated cyclization to C1-functionalized pyrano[4,3-c]pyridin-3-ones. We have also applied the outlined synthetic methodologies to the preparation of potential semi-rigid analogs of antihistamines. In the experiment, the researchers used many compounds, for example, 2-Bromonicotinaldehyde(cas: 128071-75-0SDS of cas: 128071-75-0)

2-Bromonicotinaldehyde(cas: 128071-75-0) belongs to pyridine. The basicity and metallophilic high donor number of these π-deficient systems has long favored them as ligands in metal catalysis. The last decade saw pyridine assume a stronger role as functional group for directed C–H oxidation/activation.SDS of cas: 128071-75-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Category: pyridine-derivativesIn 2022 ,《Effects of 3-Pyridinylboronic acid in zebrafish enmbryos exposed to neurotoxin,1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine》 appeared in Drug and Chemical Toxicology (1977). The author of the article were Ustundag, Fumet Duygu; Unal, Ismail; Cansiz, Derya; Ustundag, Unsal Veli; Subasat, Hulya Kara; Alturfan, A. Ata; Tiber, Pinar Mega; Emekli-Alturfan, Ebru. The article conveys some information:

1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) is a neurotoxin that damages dopaminergic neurons. Zebrafish has been shown to be a suitable model organism to investigate the mol. pathways in the pathogenesis of Parkinson disease and also for potential therapeutic agent research. Boron has been shown to play an important role in the neural activity of the brain. Boronic acids are used in combinatorial approaches in drug design and discovery. The effect of 3-pyridinylboronic acid which is an important sub-class of heterocyclic boronic acids has not been evaluated in case of MPTP exposure in zebrafish embryos. Accordingly, this study was designed to investigate the effects of 3-pyridinylboronic acid on MPTP exposed zebrafish embryos focusing on the mol. pathways related to neurodegeneration and apoptosis by RT-PCR. Zebrafish embryos were exposed to MPTP (800μM); MPTP + Low Dose 3-Pyridinylboronic acid (50μM) (MPTP + LB) and MPTP + High Dose 3-Pyridinylboronic acid (100μM) (MPTP + HB) in well plates for 72 h post fertilization. Results of our study showed that MPTP induced a P53 dependent and Bax mediated apoptosis in zebrafish embryos and 3-pyridinylboronic acid restored the locomotor activity and gene expressions related to mitochondrial dysfunction and oxidative stress due to the deleterious effects of MPTP, in a dose-dependent manner. The experimental process involved the reaction of Pyridin-3-ylboronic acid(cas: 1692-25-7Category: pyridine-derivatives)

Pyridin-3-ylboronic acid(cas: 1692-25-7) belongs to pyridine. Pyridine and pyridine-derived structures are privileged pharmacophores in medicinal chemistry and an essential functionality for organic chemists. As the prototypical π-deficient heterocycle, pyridine illustrates distinctive chemistry as both substrate and reagent. Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Safety of 4-CyanopyridineIn 2020 ,《Niacin as a Potent Organocatalyst towards the Synthesis of Quinazolines Using Nitriles as C-N Source》 appeared in European Journal of Organic Chemistry. The author of the article were Gujjarappa, Raghuram; Vodnala, Nagaraju; Reddy, Velma Ganga; Malakar, Chandi C.. The article conveys some information:

An efficient and cost-effective Vitamin-B3-catalyzed protocol towards the synthesis of diversely substituted quinazolines is illustrated using 2-aminobenzylamines and nitriles as substrates. An organocatalytic transformation has been investigated where nitrile plays a role of C-N bond donor. The developed approach is applicable on a wide range of 2-aminobenzylamines and nitriles for the synthesis of substituted quinazolines in high yields with a broad functional group tolerance.4-Cyanopyridine(cas: 100-48-1Safety of 4-Cyanopyridine) was used in this study.

4-Cyanopyridine(cas: 100-48-1) belongs to pyridine. Pyridine and pyridine-derived structures are privileged pharmacophores in medicinal chemistry and an essential functionality for organic chemists. As the prototypical π-deficient heterocycle, pyridine illustrates distinctive chemistry as both substrate and reagent. Safety of 4-Cyanopyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Application of 29682-15-3In 2008 ,《Design, synthesis, and biological evaluation of 8-biarylquinolines: A novel class of PDE4 inhibitors》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Gallant, Michel; Chauret, Nathalie; Claveau, David; Day, Stephen; Deschenes, Denis; Dube, Daniel; Huang, Zheng; Lacombe, Patrick; Laliberte, France; Levesque, Jean-Francois; Liu, Susana; Macdonald, Dwight; Mancini, Joseph; Masson, Paul; Mastracchio, Anthony; Nicholson, Donald; Nicoll-Griffith, Deborah A.; Perrier, Helene; Salem, Myriam; Styhler, Angela; Young, Robert N.; Girard, Yves. The article conveys some information:

The structure-activity relationship of a novel series of 8-biarylquinolines, e.g., I, acting as type 4 phosphodiesterase (PDE4) inhibitors is described herein. Prototypical compounds from this series are potent and non-selective inhibitors of the four distinct PDE4 (IC50 < 10 nM) isoenzymes (A-D). In a human whole blood in vitro assay, they inhibit (IC50 < 0.5 μM) the LPS-induced release of the cytokine TNF-α. Optimized inhibitors were evaluated in vivo for efficacy in an ovalbumin-induced bronchoconstriction model in conscious guinea pigs. Their propensity to produce an emetic response was evaluated by performing pharmacokinetic studies in squirrel monkeys. This work has led to the identification of several compounds with excellent in vitro and in vivo profiles, including a good therapeutic window of efficacy over emesis. In the part of experimental materials, we found many familiar compounds, such as Methyl 5-bromopicolinate(cas: 29682-15-3Application of 29682-15-3)

Methyl 5-bromopicolinate(cas: 29682-15-3) belongs to pyridine. Pyridine and pyridine-derived structures are privileged pharmacophores in medicinal chemistry and an essential functionality for organic chemists. As the prototypical π-deficient heterocycle, pyridine illustrates distinctive chemistry as both substrate and reagent. Application of 29682-15-3

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Reference of 4,4′-Dimethyl-2,2′-bipyridineIn 2020 ,《A Multi-action and Multi-target RuII-PtIV Conjugate Combining Cancer-Activated Chemotherapy and Photodynamic Therapy to Overcome Drug Resistant Cancers》 was published in Angewandte Chemie, International Edition. The article was written by Karges, Johannes; Yempala, Thirumal; Tharaud, Mickael; Gibson, Dan; Gasser, Gilles. The article contains the following contents:

PtII complexes are commonly used to treat cancer. To reduce their side effects and improve their pharmacol. properties, PtIV complexes are being developed as prodrug candidates that are activated by reduction in cancer cells. Concomitantly, RuII polypyridine complexes have gained much attention as photosensitizers for use in photodynamic therapy due to their attractive characteristics. In this article, a novel PtIV-RuII conjugate, which combines cancer activated chemotherapy with PDT, is presented. Upon entering the cancer cell, the PtIV center is reduced to PtII and the axial ligands including the RuII complex and phenylbutyrate are released. As each component has its individual targets, the conjugate exerts a multi-target and multi-action effect with (photo-)cytotoxicity values upon irradiation up to 595 nm in the low nanomolar range in various (drug resistant) 2D monolayer cancer cells and 3D multicellular tumor spheroids. In the experiment, the researchers used many compounds, for example, 4,4′-Dimethyl-2,2′-bipyridine(cas: 1134-35-6Reference of 4,4′-Dimethyl-2,2′-bipyridine)

4,4′-Dimethyl-2,2′-bipyridine(cas: 1134-35-6) is used in the synthesis of a series of o-phenanthroline-substituted ruthenium(II) complexes.Reference of 4,4′-Dimethyl-2,2′-bipyridine Furthermore, 4,4′-Dimethyl-2,2′-bipyridine is used as a chemical Intermediate. It can be used for the determination of ferrous and cyanide compounds.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

SDS of cas: 1134-35-6In 2020 ,《Rationally Designed Long-Wavelength Absorbing Ru(II) Polypyridyl Complexes as Photosensitizers for Photodynamic Therapy》 was published in Journal of the American Chemical Society. The article was written by Karges, Johannes; Heinemann, Franz; Jakubaszek, Marta; Maschietto, Federica; Subecz, Chloe; Dotou, Mazzarine; Vinck, Robin; Blacque, Olivier; Tharaud, Mickael; Goud, Bruno; Vinuelas Zahinos, Emilio; Spingler, Bernhard; Ciofini, Ilaria; Gasser, Gilles. The article contains the following contents:

The utilization of photodynamic therapy (PDT) for the treatment of various types of cancer has gained increasing attention over the last decades. Despite the clin. success of approved photosensitizers (PSs), their application is sometimes limited due to poor water solubility, aggregation, photodegradation, and slow clearance from the body. To overcome these drawbacks, research efforts are devoted toward the development of metal complexes and especially Ru(II) polypyridine complexes based on their attractive photophys. and biol. properties. Despite the recent research developments, the vast majority of complexes utilize blue or UV-A light to obtain a PDT effect, limiting the penetration depth inside tissues and, therefore, the possibility to treat deep-seated or large tumors. To circumvent these drawbacks, we present the first example of a DFT guided search for efficient PDT PSs with a substantial spectral red shift toward the biol. spectral window. Thanks to this design, we have unveiled a Ru(II) polypyridine complex that causes phototoxicity in the very low micromolar to nanomolar range at clin. relevant 595 nm, in monolayer cells as well as in 3D multicellular tumor spheroids.4,4′-Dimethyl-2,2′-bipyridine(cas: 1134-35-6SDS of cas: 1134-35-6) was used in this study.

4,4′-Dimethyl-2,2′-bipyridine(cas: 1134-35-6) is used in the synthesis of a series of o-phenanthroline-substituted ruthenium(II) complexes.SDS of cas: 1134-35-6 Furthermore, 4,4′-Dimethyl-2,2′-bipyridine is used as a chemical Intermediate. It can be used for the determination of ferrous and cyanide compounds.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Reference of 5-Bromo-2-chloropyridineIn 2013 ,《Discovery of SAR184841, a potent and long-lasting inhibitor of 11β-hydroxysteroid dehydrogenase type 1, active in a physiopathological animal model of T2D》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Venier, Olivier; Pascal, Cecile; Braun, Alain; Namane, Claudie; Mougenot, Patrick; Crespin, Olivier; Pacquet, Francois; Mougenot, Cecile; Monseau, Catherine; Onofri, Benedicte; Dadji-Faihun, Rommel; Leger, Celine; Ben-Hassine, Majdi; Van-Pham, Thao; Ragot, Jean-Luc; Philippo, Christophe; Farjot, Geraldine; Noah, Lionel; Maniani, Karima; Boutarfa, Asma; Nicolai, Eric; Guillot, Etienne; Pruniaux, Marie-Pierre; Gussregen, Stefan; Engel, Christian; Coutant, Anne-Laure; de Miguel, Beatriz; Castro, Antonio. The article contains the following contents:

Starting from 11β-HSD1 inhibitors that were active ex vivo but with Cyp 3A4 liability, we obtained a new series of adamantane ureas displaying potent inhibition of both human and rodent 11β-HSD1 enzymes, devoid of Cyp 3A4 interactions, and rationally designed to provide long-lasting inhibition in target tissues. Final optimizations lead to SAR184841 with good oral pharmacokinetic properties showing in vivo activity and improvement of metabolic parameters in a physiopathol. model of type 2 diabetes. After reading the article, we found that the author used 5-Bromo-2-chloropyridine(cas: 53939-30-3Reference of 5-Bromo-2-chloropyridine)

5-Bromo-2-chloropyridine(cas: 53939-30-3) belongs to pyridine. Pyridine and pyridine-derived structures are privileged pharmacophores in medicinal chemistry and an essential functionality for organic chemists. As the prototypical π-deficient heterocycle, pyridine illustrates distinctive chemistry as both substrate and reagent. Reference of 5-Bromo-2-chloropyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Name: 2-Bromo-5-methylpyridineIn 2019 ,《Anti-Markovnikov Hydroamination of Unactivated Alkenes with Primary Alkyl Amines》 was published in Journal of the American Chemical Society. The article was written by Miller, David C.; Ganley, Jacob M.; Musacchio, Andrew J.; Sherwood, Trevor C.; Ewing, William R.; Knowles, Robert R.. The article contains the following contents:

A photocatalytic method for the intermol. anti-Markovnikov hydroamination of unactivated olefins with primary alkyl amines to selectively furnish secondary amine products is reported. These reactions proceed through aminium radical cation (ARC) intermediates and occur at room temperature under visible light irradiation in the presence of an iridium photocatalyst and an aryl thiol hydrogen atom donor. Despite the presence of excess olefin, high selectivities are observed for secondary over tertiary amine products, even though the secondary amines are established substrates for ARC-based olefin amination under similar conditions.2-Bromo-5-methylpyridine(cas: 3510-66-5Name: 2-Bromo-5-methylpyridine) was used in this study.

2-Bromo-5-methylpyridine(cas: 3510-66-5) belongs to pyridine. Pyridine and pyridine-derived structures are privileged pharmacophores in medicinal chemistry and an essential functionality for organic chemists. As the prototypical π-deficient heterocycle, pyridine illustrates distinctive chemistry as both substrate and reagent. Name: 2-Bromo-5-methylpyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Reference of 2,5-DibromopyridineIn 2020 ,《Exploration of the Solid-State Sorption Properties of Shape-Persistent Macrocyclic Nanocarbons as Bulk Materials and Small Aggregates》 was published in Journal of the American Chemical Society. The article was written by Schaub, Tobias A.; Prantl, Ephraim A.; Kohn, Julia; Bursch, Markus; Marshall, Checkers R.; Leonhardt, Erik J.; Lovell, Terri C.; Zakharov, Lev N.; Brozek, Carl K.; Waldvogel, Siegfried R.; Grimme, Stefan; Jasti, Ramesh. The article contains the following contents:

Porous mol. materials combine benefits such as convenient processability and the possibility for atom-precise structural fine-tuning which makes them remarkable candidates for specialty applications in the areas of gas separation, catalysis, and sensing. In order to realize the full potential of these materials and guide future mol. design, knowledge of the transition from mol. properties into materials behavior is essential. In this work, the class of compounds termed cycloparaphenylenes (CPPs)-shape-persistent macrocycles with built-in cavities and radially oriented π-systems-was selected as a conceptually simple class of intrinsically porous nanocarbons to serve as a platform for studying the transition from analyte sorption properties of small aggregates to those of bulk materials. In our detailed investigation, two series of CPPs were probed: previously reported hoop-shaped [n]CPPs and a novel family of all-phenylene figure-8 shaped (lemniscal) bismacrocycles, termed spiro[n,n]CPPs. A series of nanocarbons with different macrocycle sizes and heteroatom content have been prepared by atom-precise organic synthetic methods, and their structural, photophys., and electronic attributes were disclosed. Detailed exptl. studies (X-ray crystallog., gas sorption, and quartz-crystal microbalance measurements) and quantum chem. calculations provided ample evidence for the importance of the solid-state arrangement on the porosity and analyte uptake ability of intrinsically porous mol. nanocarbons. We demonstrate that this mol. design principle, i.e., incorporation of sterically demanding spiro junctions into the backbone of nanohoops, enables the manipulation of solid-state morphol. without significantly changing the nature and size of the macrocyclic cavities. As a result, the novel spiro[n,n]CPPs showed a remarkable performance as high affinity material for vapor analyte sensing. The experimental process involved the reaction of 2,5-Dibromopyridine(cas: 624-28-2Reference of 2,5-Dibromopyridine)

2,5-Dibromopyridine(cas: 624-28-2) belongs to pyridine. Pyridines, quinolines, and isoquinolines have found a function in almost all aspects of organic chemistry. Pyridine has found use as a solvent, base, ligand, functional group, and molecular scaffold. As structural elements, these moieties are potent electron-deficient groups, metal-directing functionalities, fluorophores, and medicinally important pharmacophores. Reference of 2,5-Dibromopyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Quality Control of Pyridin-3-ylboronic acidIn 2020 ,《Chan-Evans-Lam N1-(het)arylation and N1-alkenylation of 4-fluoroalkylpyrimidin-2(1H)-ones》 was published in Beilstein Journal of Organic Chemistry. The article was written by Tkachuk, Viktor M.; Lukianov, Oleh O.; Vovk, Mykhailo V.; Gillaizeau, Isabelle; Sukach, Volodymyr A.. The article contains the following contents:

The Chan-Evans-Lam reaction of 1-unsubstituted 4-fluoroalkylpyrimidin-2(1H)-ones with arylboronic acids was reported as a facile synthetic route to hitherto unavailable N1-(het)aryl and N1-alkenyl derivatives of the corresponding pyrimidines I [R = CH=CH2, Ph, 3-thienyl, etc.; R1 = CHF2, CF3, C2F5, CClF2; R2 = H, Br, CO2Me]. An efficient C-N bond-forming process was also observed by using boronic acid pinacol esters as coupling partners in the presence of Cu(II) acetate and boric acid. The 4-fluoroalkyl group on the pyrimidine ring significantly assists in the formation of the target N1-substituted products, in contrast to the 4-Me and 4-unsubstituted substrates which did not undergo N1-arylation under similar reaction conditions. In the experiment, the researchers used Pyridin-3-ylboronic acid(cas: 1692-25-7Quality Control of Pyridin-3-ylboronic acid)

Pyridin-3-ylboronic acid(cas: 1692-25-7) belongs to pyridine. Pyridines, quinolines, and isoquinolines have found a function in almost all aspects of organic chemistry. Pyridine has found use as a solvent, base, ligand, functional group, and molecular scaffold. As structural elements, these moieties are potent electron-deficient groups, metal-directing functionalities, fluorophores, and medicinally important pharmacophores. Quality Control of Pyridin-3-ylboronic acid

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem