Day: October 19, 2022

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

SDS of cas: 29682-15-3In 2013 ,《Structural Basis and SAR for G007-LK, a Lead Stage 1,2,4-Triazole Based Specific Tankyrase 1/2 Inhibitor》 was published in Journal of Medicinal Chemistry. The article was written by Voronkov, Andrew; Holsworth, Daniel D.; Waaler, Jo; Wilson, Steven R.; Ekblad, Bie; Perdreau-Dahl, Harmonie; Dinh, Huyen; Drewes, Gerard; Hopf, Carsten; Morth, Jens P.; Krauss, Stefan. The article contains the following contents:

Tankyrases 1 and 2 (TNKS1/2) are promising pharmacol. biotargets with possible applications for the development of novel anticancer therapeutics. A focused structure-activity relationship study was conducted based on the tankyrase inhibitor JW74 (1). Chem. analoging of 1 improved the 1,2,4-triazole based core and led to 4-{5-[(E)-2-{4-(2-chlorophenyl)-5-[5-(methylsulfonyl)pyridin-2-yl]-4H-1,2,4-triazol-3-yl}ethenyl]-1,3,4-oxadiazol-2-yl}benzonitrile (G007-LK), a potent, “”rule of 5″” compliant and a metabolically stable TNKS1/2 inhibitor. G007-LK (66) displayed high selectivity toward tankyrases 1 and 2 with biochem. IC50 values of 46 nM and 25 nM, resp., and a cellular IC50 value of 50 nM combined with an excellent pharmacokinetic profile in mice. The PARP domain of TNKS2 was cocrystd. with 66, and the X-ray structure was determined at 2.8 Å resolution in the space group P3221. The structure revealed that 66 binds to unique structural features in the extended adenosine binding pocket which forms the structural basis for the compound’s high target selectivity and specificity. Our study provides a significantly optimized compound for targeting TNKS1/2 in vitro and in vivo. After reading the article, we found that the author used Methyl 5-bromopicolinate(cas: 29682-15-3SDS of cas: 29682-15-3)

Methyl 5-bromopicolinate(cas: 29682-15-3) 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. SDS of cas: 29682-15-3

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

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

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

《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

《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

《Grafting Modification of Poly(vinylidene fluoride-trifluoroethylene) via Visible-Light Mediated C-F Bond Activation》 was written by Wang, Miao; Lei, Mingxin; Tan, Shaobo; Zhang, Zhicheng. Safety of fac-Tris(2-phenylpyridine)iridiumThis research focused onvinylidene fluoride trifluoroethylene copolymer graft polymerization bond activation. The article conveys some information:

In this work, a strategy of C-F bond activation for grafting modification of poly(vinylidene fluoride-trifluoroethylene) (h-P(VDF-TrFE), TrFE is dominantly as -CF2CH2-CFHCF2- sequence) using an Ir-based photoredox catalyst is reported. The graft polymerization exhibits first-order kinetics, and the chem. composition of the graft copolymer can be easily adjusted by changing the reaction conditions. Importantly, the side reaction of dehydrofluorination (β-H elimination) can be effectively avoided, which occurs in the previously reported copper complex catalytic system. Moreover, the purification process is greatly simplified due to the extremely low content of catalyst added. This work may provide a facile strategy for incorporating functional groups into h-P(VDF-TrFE) via directly activating C-F bond under mild conditions. In the experimental materials used by the author, we found fac-Tris(2-phenylpyridine)iridium(cas: 94928-86-6Safety of fac-Tris(2-phenylpyridine)iridium)

fac-Tris(2-phenylpyridine)iridium(cas: 94928-86-6) 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.Safety of fac-Tris(2-phenylpyridine)iridium

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

《One-Pot Direct Synthesis of Weinreb Amides From Aryl and Hetero Aryl Halides Using Co2(CO)8 as an Effective CO Source Under Conventional Thermal Heating》 was written by Baburajan, Poongavanam; Elango, Kuppanagounder P.. Safety of 5-Bromo-2-chloropyridineThis research focused onWeinreb amide cobalt carbonyl reaction; aminocarbonylation aryl halide cobalt carbonyl. The article conveys some information:

A successful protocol for the synthesis of Weinreb amides directly from aryl halides via aminocarbonylation with N,O-dimethylhydroxylamine using Co2(CO)8 as an in situ CO source has been demonstrated. The effects of various reaction parameters such as temperature, base, and CO source have also been investigated and optimized. In the experimental materials used by the author, we found 5-Bromo-2-chloropyridine(cas: 53939-30-3Safety of 5-Bromo-2-chloropyridine)

5-Bromo-2-chloropyridine(cas: 53939-30-3) 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.Safety of 5-Bromo-2-chloropyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Synthetic Route of C6H6ClNO2SOn September 10, 2020 ,《Identification and Optimization of Pyrrolidine Derivatives as Highly Potent Ghrelin Receptor Full Agonists》 was published in Journal of Medicinal Chemistry. The article was written by Cooper, Martin; Llinas, Antonio; Hansen, Peter; Caffrey, Moya; Ray, Asim; Sjoedin, Stina; Shamovsky, Igor; Wada, Hiroki; Jellesmark Jensen, Tina; Sivars, Ulf; Hultin, Leif; Andersson, Ulf; Lundqvist, Sara; Gedda, Karin; Jinton, Lisa; Krutroek, Nina; Lewis, Richard; Jansson, Paul; Gardelli, Cristina. The article contains the following contents:

Muscle atrophy and cachexia are common comorbidities among patients suffering from cancer, chronic obstructive pulmonary disease, and several other chronic diseases. The peptide hormone ghrelin exerts pleiotropic effects including the stimulation of growth hormone secretion and subsequent increase of insulin-like growth factor-1 levels, an important mediator of muscle growth and repair. Ghrelin also acts on inflammation, appetite, and adipogenesis and therefore has been considered a promising therapeutic target for catabolic conditions. We previously reported on the synthesis and properties of an indane based series of ghrelin receptor full agonists which led to a sustained increase of insulin-like growth factor-1 in a dog pharmacodynamic study. Herein we report on the identification of a series of pyrrolidine or piperidine based full agonists and attempted optimization to give compounds with profiles suitable for progression as clin. candidates. In the part of experimental materials, we found many familiar compounds, such as 2-Methylpyridine-4-sulfonyl chloride(cas: 1025509-77-6Synthetic Route of C6H6ClNO2S)

2-Methylpyridine-4-sulfonyl chloride(cas: 1025509-77-6) 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.Synthetic Route of C6H6ClNO2S

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem