Tag: 100-200

《Oxidative ammonolysis of β- and γ-picoline on modified vanadium-titanium oxide catalysts》 was written by Vorobyev, P. B.; Mikhailovskaya, T. P.; Kadirbekov, K. A.; Kurmakyzy, R.. Application of 100-48-1This research focused onvanadium titanium chromium tin iron oxide oxidative ammonolysis catalyst; nicotinonitrile isonicotinonitrile preparation; selectivity vanadium titanium oxide catalyst oxidative ammonolysis picoline. The article conveys some information:

The modifying effect of chromium (III), tin (IV) and iron (III) oxide additives to the binary V-Ti-oxide system in the reaction of oxidative ammonolysis of β- and γ-picolines was investigated. Relation of the studied oxide systems catalytic activity on the calculated values of proton affinity for the vanadyl oxygen of their surface, which is involved in the deprotonation of Me substituents converted to a nitrile group, has been established. The experimental part of the paper was very detailed, including the reaction process of 4-Cyanopyridine(cas: 100-48-1Application of 100-48-1)

4-Cyanopyridine(cas: 100-48-1) belongs to pyridine. Pyridine-based materials are valued for their optical and physical properties as well as their medical potential. Additionally, pyridine-based natural products continue to be discovered and studied for their properties and to understand their biosynthesis.Application of 100-48-1

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

《Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design》 was written by Cheng, Hengmiao; Li, Chunze; Bailey, Simon; Baxi, Sangita M.; Goulet, Lance; Guo, Lisa; Hoffman, Jacqui; Jiang, Ying; Johnson, Theodore Otto; Johnson, Ted W.; Knighton, Daniel R.; Li, John; Liu, Kevin K.-C.; Liu, Zhengyu; Marx, Matthew A.; Walls, Marlena; Wells, Peter A.; Yin, Min-Jean; Zhu, Jinjiang; Zientek, Michael. Category: pyridine-derivativesThis research focused ontricyclic imidazonaphthyridine preparation PI3K mTOR dual kinase inhibitor; PF-04979064; PI3K/mTOR dual inhibitor; aldehyde oxidase metabolism; antitumor; cancer; kinase inhibitor. The article conveys some information:

PI3K, AKT, and mTOR are key kinases from PI3K signaling pathway being extensively pursued to treat a variety of cancers in oncol. To search for a structurally differentiated back-up candidate to PF-04691502, which is currently in phase I/II clin. trials for treating solid tumors, a lead optimization effort was carried out with a tricyclic imidazo[1,5]naphthyridine series. Integration of structure-based drug design and phys. properties-based optimization yielded a potent and selective PI3K/mTOR dual kinase inhibitor PF-04979064 (I). This manuscript discusses the lead optimization for the tricyclic series, which both improved the in vitro potency and addressed a number of ADMET issues including high metabolic clearance mediated by both P 450 and aldehyde oxidase (AO), poor permeability, and poor solubility An empirical scaling tool was developed to predict human clearance from in vitro human liver S9 assay data for tricyclic derivatives that were AO substrates. In the experiment, the researchers used many compounds, for example, 6-Bromopyridin-3-amine(cas: 13534-97-9Category: pyridine-derivatives)

6-Bromopyridin-3-amine(cas: 13534-97-9) belongs to anime. Milder oxidation, using reagents such as NaOCl, can remove four hydrogen atoms from primary amines of the type RCH2NH2 to form nitriles (R―C≡N), and oxidation with reagents such as MnO2 can remove two hydrogen atoms from secondary amines (R2CH―NHR′) to form imines (R2C=NR′). Tertiary amines can be oxidized to enamines (R2C=CHNR2) by a variety of reagents.Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

《Diminishing GSH-Adduct Formation of Tricyclic Diazepine-based Mutant IDH1 Inhibitors》 was written by Huang, Chunhui; Fischer, Christian; Machacek, Michelle R.; Bogen, Stephane; Biftu, Tesfaye; Huang, Xianhai; Reutershan, Michael H.; Otte, Ryan; Hong, Qingmei; Wu, Zhicai; Yu, Yang; Park, Min; Chen, Lei; Biju, Purakkattle; Knemeyer, Ian; Lu, Ping; Kochansky, Christopher J.; Hicks, Michael Brendan; Liu, Yong; Helmy, Roy; Fradera, Xavier; Donofrio, Anthony; Close, Josh; Maddess, Matthew L.; White, Catherine; Sloman, David L.; Sciammetta, Nunzio; Lu, Jun; Gibeau, Craig; Simov, Vladimir; Zhang, Hongjun; Fuller, Peter; Witter, David. Recommanded Product: 128071-75-0This research focused ontricyclic diazepine preparation SAR mutant isocitrate dehydrogenase inhibitor. The article conveys some information:

Efforts to reduce the electron-rich nature of the core were described. Ultimately, a strategy focused on core modifications to block metabolic hot spots coupled with substitution pattern changes (C8 N → C linked) led to the identification of new tricyclic analogs such as I (R1 = 1-aza-4-oxa[2.2.2]bicyclooctyl; R2 = trans-4-isopropoxycyclohexyl) with minimal GSH-adduct formation across species while maintaining an overall balanced profile.2-Bromonicotinaldehyde(cas: 128071-75-0Recommanded Product: 128071-75-0) was used in this study.

2-Bromonicotinaldehyde(cas: 128071-75-0) belongs to pyridine. Pyridine-based materials are valued for their optical and physical properties as well as their medical potential. Additionally, pyridine-based natural products continue to be discovered and studied for their properties and to understand their biosynthesis.Recommanded Product: 128071-75-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Quality Control of 2-BromonicotinaldehydeIn 2018 ,《Thiobarbiturates as potential antifungal agents to control human infections caused by Candida and Cryptococcus species》 was published in Medicinal Chemistry Research. The article was written by Shabeer, Muhammad; Barbosa, Luiz C. A.; Karak, Milandip; Coelho, Amanda C. S.; Takahashi, Jacqueline A.. The article contains the following contents:

Hospitalized patients can suffer from Candida and Crytptococcus infections, aggravating underlying health conditions. Due to the development of drug-resistant microorganisms, we report here on the potential of some arylidene-thiobarbiturate to control five Candida spp. and one Cryptococcus species of medical interest. Initially, a bismuth nitrate catalyzed Knoevenagel condensation with thiobarbituric acid and aromatic aldehydes was developed. This new procedure generated seven new and thirteen known arylidene-thiobarbiturate derivatives (1-20) with excellent yields (81-95%), with a reaction time within 20 min. The antimicrobial activities of all compounds were evaluated against Candida albicans, C. tropicalis, C. parapsilosis, C. lusitaniae, C. dubliniensis, and Cryptococcus neoformans. Several compounds were as active as the com. available drugs (IC50 < 1.95 μg mL-1) towards at least one microbial strain. The results suggest that some of the new compounds can serve as leads for new antimicrobial agents for the treatment of human fungal infections. In the experiment, the researchers used many compounds, for example, 2-Bromonicotinaldehyde(cas: 128071-75-0Quality Control of 2-Bromonicotinaldehyde)

2-Bromonicotinaldehyde(cas: 128071-75-0) 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 2-Bromonicotinaldehyde

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Quality Control of Picolinic acidIn 2019 ,《Thermochemistry of the Acid-Base Interactions in Aqueous Solutions of Isonicotinic and Picolinic Acids》 was published in Russian Journal of General Chemistry. The article was written by Lytkin, A. I.; Badelin, V. G.; Krutova, O. N.; Tyunina, E. Yu.; Krutov, P. D.. The article contains the following contents:

The calorimetric method was employed to measure the heat effects of the interaction of isonicotinic and picolinic acids with HNO3 in aqueous solutions over different pH ranges at 298.15 K and ionic strengths of 0.5, 1.0, and 1.5 against potassium nitrate. The heat effects of stepwise dissociation of the acids were determined The standard thermodn. characteristics (ΔrH°, ΔrG°, ΔrS°, ΔCp°) of the acid-base reactions in aqueous solutions of isonicotinic and picolinic acids were calculated The results came from multiple reactions, including the reaction of Picolinic acid(cas: 98-98-6Quality Control of Picolinic acid)

Picolinic acid(cas: 98-98-6) is used as a chelate for alkaline earth metals. Used to prepare picolinato ligated transition metal complexes. In synthetic organic chemistry, has been used as a substrate in the Mitsunobu reaction and in the Hammick reaction.Quality Control of Picolinic acid

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Related Products of 103-74-2In 2018 ,《Solid-Phase Synthesis of Tetramic Acid via Resin-Bound Enol Ethers as a Privileged Scaffold in Drug Discovery》 was published in Advanced Synthesis & Catalysis. The article was written by Schuetznerova, Eva; Oliver, Allen G.; Pribylka, Adam; Krchnak, Viktor. The article contains the following contents:

This paper reports the practical synthesis of a tetramic acid scaffold on solid phase using simple, com. available building blocks under mild conditions. Acyclic precursors were assembled on solid phase in four steps, and cyclization was achieved by Wittig olefination. The target compounds contained three points of diversification and allowed for further modifications while still being attached to the resin. Solid-phase synthesis represents a method of choice, particularly for parallel synthesis, because the intermediates can be isolated simply and quickly by washing the resin beads, which typically takes only minutes.2-(2-Hydroxyethyl)pyridine(cas: 103-74-2Related Products of 103-74-2) was used in this study.

2-(2-Hydroxyethyl)pyridine(cas: 103-74-2) 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. Related Products of 103-74-2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Reference of 4-CyanopyridineIn 2020 ,《Arene-ruthenium(II)-phosphine complexes: Green catalysts for hydration of nitriles under mild conditions》 was published in Inorganic Chemistry Communications. The article was written by Vyas, Komal M.; Mandal, Poulami; Singh, Rinky; Mobin, Shaikh M.; Mukhopadhyay, Suman. The article contains the following contents:

Three new arene-ruthenium(II) complexes were prepared by treating [{RuCl(μ-Cl)(η6-arene)}2] (η6-arene = p-cymene) dimer with tri(2-furyl)phosphine (PFu3) and 1,3,5-triaza-7-phosphaadamantane (PTA), resp. to obtain [RuCl2(η6-arene)PFu3] [Ru]-1, [RuCl(η6-arene)(PFu3)(PTA)]BF4 [Ru]-2 and [RuCl(η6-arene)(PFu3)2]BF4 [Ru]-3. All the complexes were structurally identified using anal. and spectroscopic methods including single-crystal X-ray studies. The effectiveness of resulting complexes as potential homogeneous catalysts for selective hydration of different nitriles into corresponding amides in aqueous medium and air atm. was explored. There was a remarkable difference in catalytic activity of the catalysts depending on the nature and number of phosphorus-donor ligands and sites available for catalysis. Exptl. studies performed using structural analogs of efficient catalyst concluded a structural-activity relationship for the higher catalytic activity of [Ru]-1, being able to convert huge variety of aromatic, heteroaromatic and aliphatic nitriles. The use of eco-friendly water as a solvent, open atm. and avoidance of any organic solvent during the catalytic reactions prove the reported process to be truly green and sustainable. After reading the article, we found that the author used 4-Cyanopyridine(cas: 100-48-1Reference of 4-Cyanopyridine)

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. Reference of 4-Cyanopyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Recommanded Product: 1692-25-7In 2020 ,《Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity》 appeared in European Journal of Medicinal Chemistry. The author of the article were Teng, Yu; Li, Xinyu; Ren, Shengnan; Cheng, Yu; Xi, Kun; Shen, Hongtao; Ma, Wenzhuo; Luo, Guoshun; Xiang, Hua. The article conveys some information:

Herein, a series of quinazoline derivatives I [R1 = Br, 3-pyridyl, (6-fluoro-3-pyridyl), (6-chloro-3-pyridyl), 3-quinolyl; R2 = vinyl, Et, HC=CH2CH3, C≡CCH3; R3 = H, Me] bearing acrylamide fragment were prepared using skeleton-deconstruction strategy. The preliminary bioactivity evaluation resulted in the discovery of lead compound I [R1 = 3-quinolyl; R2 = vinyl; R3 = Me]. Compound I [R1 = 3-quinolyl; R2 = vinyl; R3 = Me] exhibited excellent enzyme activity against PI3Kδ (IC50 = 27.5 nM) compared with BEZ235 as well as the significant anti-proliferation activities. With the high selectivity over other PI3K isoforms and potent effects on PI3K/Akt pathway, compoundI [R1 = 3-quinolyl; R2 = vinyl; R3 = Me] could be identified as a promising PI3Kδ inhibitor worthy of further profiling. The experimental process involved the reaction of Pyridin-3-ylboronic acid(cas: 1692-25-7Recommanded Product: 1692-25-7)

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. Recommanded Product: 1692-25-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

COA of Formula: C7H7NOIn 2020 ,《Copper-catalyzed formal [1 + 2 + 2]-annulation of alkyne-tethered diazoacetates and pyridines: access to polycyclic indolizines》 appeared in Organic & Biomolecular Chemistry. The author of the article were Dong, Shanliang; Huang, Jingjing; Sha, Hongkai; Qiu, Lihua; Hu, Wenhao; Xu, Xinfang. The article conveys some information:

A copper-catalyzed formal [1 + 2 + 2] annulation of alkyne-tethered diazo compounds with pyridines afforded polycyclic fused indolizines in good yields under mild reaction conditions was reported. This method features the use of an inexpensive copper catalyst and readily available starting materials, broad substrate generality and operational simplicity. Notably, a variety of natural product derivatives were compatible under the current conditions, which showed significant potential of this method for the selective decoration and modification of analogous biomols. or pharmaceuticals. In the experiment, the researchers used 4-Acetylpyridine(cas: 1122-54-9COA of Formula: C7H7NO)

4-Acetylpyridine(cas: 1122-54-9) 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.COA of Formula: C7H7NO

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Application In Synthesis of 2-Pyridinylboronic acidIn 2021 ,《Scaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis》 appeared in Journal of Medicinal Chemistry. The author of the article were Thomas, Michael; Brand, Stephen; De Rycker, Manu; Zuccotto, Fabio; Lukac, Iva; Dodd, Peter G.; Ko, Eun-Jung; Manthri, Sujatha; McGonagle, Kate; Osuna-Cabello, Maria; Riley, Jennifer; Pont, Caterina; Simeons, Frederick; Stojanovski, Laste; Thomas, John; Thompson, Stephen; Viayna, Elisabet; Fiandor, Jose M.; Martin, Julio; Wyatt, Paul G.; Miles, Timothy J.; Read, Kevin D.; Marco, Maria; Gilbert, Ian H.. The article conveys some information:

There is an urgent need for new treatments for visceral leishmaniasis (VL), a parasitic infection which impacts heavily large areas of East Africa, Asia, and South America. We previously reported on the discovery of GSK3494245/DDD01305143 (1) as a preclin. candidate for VL and, herein, we report on the medicinal chem. program that led to its identification. A hit from a phenotypic screen was optimized to give a compound with in vivo efficacy, which was hampered by poor solubility and genotoxicity. The work on the original scaffold failed to lead to developable compounds, so an extensive scaffold-hopping exercise involving medicinal chem. design, in silico profiling, and subsequent synthesis was utilized, leading to the preclin. candidate. The compound was shown to act via proteasome inhibition, and we report on the modeling of different scaffolds into a cryo-EM structure and the impact this has on our understanding of the series’ structure-activity relationships. In the experiment, the researchers used many compounds, for example, 2-Pyridinylboronic acid(cas: 197958-29-5Application In Synthesis of 2-Pyridinylboronic acid)

2-Pyridinylboronic acid(cas: 197958-29-5) 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.Application In Synthesis of 2-Pyridinylboronic acid

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem