Month: October 2022

Recommanded Product: 1122-54-9In 2022 ,《Alkyl/Glycosyl Sulfoxides as Radical Precursors and Their Use in the Synthesis of Pyridine Derivatives》 appeared in Angewandte Chemie, International Edition. The author of the article were Xie, Demeng; Wang, Yingwei; Zhang, Xia; Fu, Zhengyan; Niu, Dawen. The article conveys some information:

Here the use of simple and readily available alkyl sulfoxides as precursors to radicals and their application in the preparation of pyridine derivatives are reported. It was shown that alkyl sulfoxides, N-methoxy pyridinium salts and fluoride anions form electron donor-acceptor (EDA) complexes in solution, which, upon visible light irradiation, undergo a radical chain process to afford various pyridine derivatives smoothly. This reaction displays broad scope with respect to both sulfoxides and N-methoxy pyridinium salts. The synthetic versatility of sulfoxides as a handle in chem. adds to their power as radical precursors. Glycosyl sulfoxides are converted to the corresponding pyridyl C-glycosides with high stereoselectivities. Computational and exptl. studies provide insights into the reaction mechanism. In addition to this study using 4-Acetylpyridine, there are many other studies that have used 4-Acetylpyridine(cas: 1122-54-9Recommanded Product: 1122-54-9) was used in this study.

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.Recommanded Product: 1122-54-9

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Related Products of 53939-30-3In 2019 ,《Scaffold Morphing Identifies 3-Pyridyl Azetidine Ureas as Inhibitors of Nicotinamide Phosphoribosyltransferase (NAMPT)》 appeared in ACS Medicinal Chemistry Letters. The author of the article were Palacios, Daniel S.; Meredith, Erik L.; Kawanami, Toshio; Adams, Christopher M.; Chen, Xin; Darsigny, Veronique; Palermo, Mark; Baird, Daniel; George, Elizabeth L.; Guy, Chantale; Hewett, Jeffrey; Tierney, Laryssa; Thigale, Sachin; Wang, Louis; Weihofen, Wilhelm A.. The article conveys some information:

Small mols. that inhibit the metabolic enzyme NAMPT have emerged as potential therapeutics in oncol. As part of our effort in this area, we took a scaffold morphing approach and identified 3-pyridyl azetidine ureas as a potent NAMPT inhibiting motif. We explored the SAR of this series, including 5 and 6 amino pyridines, using a convergent synthetic strategy. This lead optimization campaign yielded multiple compounds with excellent in vitro potency and good ADME properties that culminated in compound 27.5-Bromo-2-chloropyridine(cas: 53939-30-3Related Products of 53939-30-3) was used in this study.

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. Related Products of 53939-30-3

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

HPLC of Formula: 13534-97-9In 2012 ,《Discovery of 6,7-Dihydro-5H-pyrrolo[2,3-d]pyrimidines as Orally Available G Protein-Coupled Receptor 119 Agonists》 appeared in Journal of Medicinal Chemistry. The author of the article were Katamreddy, Subba R.; Carpenter, Andrew J.; Ammala, Carina E.; Boros, Eric E.; Brashear, Ron L.; Briscoe, Celia P.; Bullard, Sarah R.; Caldwell, Richard D.; Conlee, Christopher R.; Croom, Dallas K.; Hart, Shane M.; Heyer, Dennis O.; Johnson, Paul R.; Kashatus, Jennifer A.; Minick, Doug J.; Peckham, Gregory E.; Ross, Sean A.; Roller, Shane G.; Samano, Vicente A.; Sauls, Howard R.; Tadepalli, Sarva M.; Thompson, James B.; Xu, Yun; Way, James M.. The article conveys some information:

GPR119 is a 7-transmembrane receptor that is expressed in the enteroendocrine cells in the intestine and in the islets of Langerhans in the pancreas. Indolines and 6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidines were discovered as G protein-coupled receptor 119 (GPR119) agonists, and lead optimization efforts led to the identification of 1-methylethyl 4-({7-[2-fluoro-4-(methylsulfonyl)phenyl]-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)-1-piperidinecarboxylate (GSK1104252A) (3, I), a potent and selective GPR119 agonist. Compound 3 showed excellent pharmacokinetic properties and sufficient selectivity with in vivo studies supporting a role for GPR119 in glucose homeostasis in the rodent. Thus, 3 appeared to modulate the enteroinsular axis, improve glycemic control, and strengthen previous suggestions that GPR119 agonists may have utility in the treatment of type 2 diabetes. The experimental part of the paper was very detailed, including the reaction process of 6-Bromopyridin-3-amine(cas: 13534-97-9HPLC of Formula: 13534-97-9)

6-Bromopyridin-3-amine(cas: 13534-97-9) belongs to anime. Nitrous acid converts secondary amines (aliphatic or aromatic) to N-nitroso compounds (nitrosamines): R2NH + HNO2 → R2N―NO. Some nitrosamines are potent cancer-inducing substances, and their possible formation is a serious consideration when nitrites, which are salts of nitrous acid, are present in foods or pharmaceutical preparations. Tertiary amines give rise to nitrosamines more slowly; an alkyl group is eliminated as an aldehyde or ketone, along with nitrous oxide, N2O.HPLC of Formula: 13534-97-9

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Recommanded Product: 4,4′-Dimethyl-2,2′-bipyridineIn 2019 ,《Synthesis, photophysics and the binding studies of rhenium(I) diimine surfactant complexes with serum albumins: A spectroscopic and docking study approach》 appeared in Journal of Luminescence. The author of the article were Balakrishnan, Gopalakrishnan; Rajendran, Thangamuthu; Murugan, Krishnan Senthil; Ganesan, Muniyandi; Sivasubramanian, Veluchamy Kamaraj; Rajagopal, Seenivasan. The article conveys some information:

Synthesis of the four rhenium(I) diimine surfactant complexes of the type fac-[Re(CO)3 (α-diimine){4-C11py}] CF3SO31a-1d (α-diimine = 2,2′-bipyridine) (a), 4,4′-di-methyl-2,2′-bipyridine (b), 4,4′-di-tert-butyl-2,2′-bipyridine (c) 4,4′-dinonyl-2,2′-bipyridine (d) and 4-C11py = (py-4-(CH2)10CH3) has been reported. In vitro protein (HSA and BSA) binding studies confirmed the binding affinity of the complexes toward the drug binding sites of subdomain IIA and IIIA, confirmed by spectral studies and mol. docking. The steady-state and time-resolved fluorescence spectra confirm that the static quenching, due to complex formation, is the dominant mechanism for fluorescence quenching. Mol. docking studies prove that hydrophobic interaction makes a predominant contribution even though hydrogen bonding does exist, and hence 1b, 1c and 1d exhibit stronger binding relative to 1a. The synchronous fluorescence and CD spectral studies show that these Re(I) complexes can induce conformational changes in the proteins. Finally, the distance, r, between donor (proteins) and acceptor (Re (I) complexes) obtained through FRET study is in the range 4.5-5.2 nm. The results came from multiple reactions, including the reaction of 4,4′-Dimethyl-2,2′-bipyridine(cas: 1134-35-6Recommanded Product: 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.Recommanded Product: 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

COA of Formula: C5H6BNO2In 2022 ,《Ornamenting of Blue Thermally Activated Delayed Fluorescence Emitters by Anchor Groups for the Minimization of Solid-State Solvation and Conformation Disorder Corollaries in Non-Doped and Doped Organic Light-Emitting Diodes》 was published in ACS Applied Materials & Interfaces. The article was written by Mahmoudi, Malek; Gudeika, Dalius; Kutsiy, Stepan; Simokaitiene, Jurate; Butkute, Rita; Skhirtladze, Levani; Woon, Kai Lin; Volyniuk, Dmytro; Grazulevicius, Juozas Vidas. The article contains the following contents:

Motivated to minimize the effects of solid-state solvation and conformation disorder on emission properties of donor-acceptor-type emitters, we developed five new asym. multiple donor-acceptor type derivatives of tert-Bu carbazole and trifluoromethyl benzene exploiting different electron-accepting anchoring groups. Using this design strategy, for a compound containing four di-tert-Bu carbazole units as donors as well as 5-Me pyrimidine and trifluoromethyl acceptor moieties, small singlet-triplet splitting of ca. 0.03 eV, reverse intersystem crossing rate of 1 x 106 s-1, and high photoluminescence quantum yield of neat film of ca. 75% were achieved. This compound was also characterized by the high value of hole and electron mobilities of 8.9 x 10-4 and 5.8 x 10-4 cm2 V-1 s-1 at an elec. field of 4.7 x 105 V/cm, showing relatively good hole/electron balance, resp. Due to the lowest conformational disorder and solid-state solvation effects, this compound demonstrated very similar emission properties (emission colors) in non-doped and differently doped organic light-emitting diodes (OLEDs). The lowest conformational disorder was observed for the compound with the addnl. accepting moiety inducing steric hindrance, limiting donor-acceptor dihedral rotational freedom. It can be exploited in the multi-donor-acceptor approach, increasing the efficiency. Using an emitter exhibiting the minimized solid-state solvation and conformation disorder effects, the sky blue OLED with the emitting layer of this compound dispersed in host 1,3-bis(N-carbazolyl)benzene displayed an emission peak at 477 nm, high brightness over 39 000 cd/m2, and external quantum efficiency up to 15.9% along with a maximum current efficiency of 42.6 cd/A and a maximum power efficiency of 24.1 lm/W. After reading the article, we found that the author used 2-Pyridinylboronic acid(cas: 197958-29-5COA of Formula: C5H6BNO2)

2-Pyridinylboronic acid(cas: 197958-29-5) 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. COA of Formula: C5H6BNO2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

《2D and 3D Zn(II) coordination polymers based on 4′-(Thiophen-2-yl)-4,2′:6′,4”-terpyridine: Structures and features of sorption behavior》 was written by Zaguzin, Alexander S.; Mahmoudi, Ghodrat; Sukhikh, Taisia S.; Sakhapov, Ilyas F.; Zherebtsov, Dmitry A.; Zubkov, Fedor I.; Valchuk, Karina S.; Sokolov, Maxim N.; Fedin, Vladimir P.; Adonin, Sergey A.. Application of 1122-54-9This research focused onzinc terephthalate iodoterephthalate thiophenylterpyridine coordination polymer preparation gas adsorption; crystal structure zinc terephthalate iodoterephthalate thiophenylterpyridine coordination polymer. The article conveys some information:

Reactions of Zn(II) nitrate, 4′-(thiophen-2-yl)-4,2′:6′,4”-terpyridine (ThioTerPy) and terephthalic (bdc) or 2-iodoterephthalic (2-I-bdc) acids result in 2D coordination polymer [Zn2bdc(ThioTerPy)2(OH)2] (1) or 3D metal-organic framework [Zn(2-I-bdc)(ThioTerPy)] (2), resp. Both compounds were characterized by X-ray diffractometry. For 2, I2 absorption, as well as selectivity of sorption of different organic substrates from mixtures was studied. In addition to this study using 4-Acetylpyridine, there are many other studies that have used 4-Acetylpyridine(cas: 1122-54-9Application of 1122-54-9) was used in this study.

4-Acetylpyridine(cas: 1122-54-9) 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 1122-54-9

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

《Rational design of pyridyl derivatives of vanillin for the treatment of sickle cell disease》 was written by Pagare, Piyusha P.; Ghatge, Mohini S.; Musayev, Faik N.; Deshpande, Tanvi M.; Chen, Qiukan; Braxton, Courtney; Kim, Solyi; Venitz, Jurgen; Zhang, Yan; Abdulmalik, Osheiza; Safo, Martin K.. Electric Literature of C6H7Br2NThis research focused onvanillin pyridyl derivative preparation sickle cell disease treatment Hb; Antisickling; Aromatic aldehyde; Crystal structure; Hemoglobin; Oxygen equilibrium; Polymerization; Relaxed state; Sickle cell disease. The article conveys some information:

Hypoxia-induced polymerization of sickle Hb (Hb S) is the principal phenomenon that underlays the pathophysiol. and morbidity associated with sickle cell disease (SCD). Opportunely, as an allosteric protein, Hb serves as a convenient and potentially critical druggable target. Consequently, mols. that prevent Hb S polymerization (Hb modifiers), and the associated erythrocyte sickling have been investigated-and retain significant interest-as a viable therapeutic strategy for SCD. This group of mols., including aromatic aldehydes, form high oxygen affinity Schiff-base adducts with Hb S, which are resistant to polymerization Here, the authors report the design and synthesis of novel potent antisickling agents (SAJ-009, SAJ-310 and SAJ-270) based on the pharmacophore of vanillin and INN-312, a previously reported pyridyl derivative of vanillin. These novel derivatives exhibited superior in vitro binding and pharmacokinetic properties compared to vanillin, which translated into significantly enhanced allosteric and antisickling properties. Crystal structure studies of liganded Hb in the R2 quaternary state in complex with SAJ-310 provided important insights into the allosteric and antisickling properties of this group of compounds While these derivatives generally show similar in vitro biol. potency, significant structure-dependent differences in their biochem. profiles would help predict the most promising candidates for successful in vivo pre-clin. translational studies and inform further structural modifications to improve on their pharmacol. properties. The experimental part of the paper was very detailed, including the reaction process of 2-(Bromomethyl)pyridine hydrobromide(cas: 31106-82-8Electric Literature of C6H7Br2N)

2-(Bromomethyl)pyridine hydrobromide(cas: 31106-82-8) 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.Electric Literature of C6H7Br2N

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Application In Synthesis of 4,4′-Bis(chloromethyl)-2,2′-bipyridineOn October 24, 2018 ,《Extending Hypochlorite Sensing from Cells to Elesclomol-Treated Tumors in Vivo by Using a Near-Infrared Dual-Phosphorescent Nanoprobe》 was published in ACS Applied Materials & Interfaces. The article was written by Meng, Xiangchun; Shi, Yuxiang; Chen, Zejing; Song, Linna; Zhao, Menglong; Zou, Liang; Liu, Shujuan; Huang, Wei; Zhao, Qiang. The article contains the following contents:

Reactive oxygen species (ROS), when beyond the threshold, can exhaust the capacity of cellular antioxidants and ultimately trigger cell apoptosis in tumor biol. However, the roles of hypochlorite (ClO-) in this process are much less clear compared with those of ROS, and its detection is easily obstructed by tissue penetration and endogenous fluorophores. Herein, the authors first synthesized a near-IR (NIR) ratiometric ClO- probe (Ir NP) composed of two kinds of phosphorescent iridium(III) complexes (Ir1 and Ir2) encapsulated with amphiphilic DSPE-mPEG5000. Ir NPs are dual-emissive and show obvious changes in phosphorescence intensity ratios and lifetimes of two emission bands upon exposure to ClO-. During the ClO- detection, ratiometric photoluminescence imaging is much more reliable over the intensity-based one for its self-calibration, while time-resolved photoluminescence imaging (TRPI) could distinguish the phosphorescence with long lifetime of Ir NPs from short-lived autofluorescence of tissues, resulting in the high accuracy of ClO- determination With NIR emission, a long phosphorescence lifetime, fast response, and excellent biocompatibility, Ir NPs were applied to the detection of ClO- in vitro and in vivo by means of ratiometric phosphorescence imaging and TRPI with high signal-to noise-ratios (SNR). Importantly, the authors demonstrated the elevated ClO- in elesclomol-stimulated tumors in living mice for the first time, which holds great potential for the visualization of the boost of ClO- in anticarcinogen-treated tumors and the further investigation of ROS-related oncotherapeutics. The experimental process involved the reaction of 4,4′-Bis(chloromethyl)-2,2′-bipyridine(cas: 138219-98-4Application In Synthesis of 4,4′-Bis(chloromethyl)-2,2′-bipyridine)

4,4′-Bis(chloromethyl)-2,2′-bipyridine(cas: 138219-98-4) belongs to pyridine derivatives. Several pyridine derivatives play important roles in biological systems. While its biosynthesis is not fully understood, nicotinic acid (vitamin B3) occurs in some bacteria, fungi, and mammals. Application In Synthesis of 4,4′-Bis(chloromethyl)-2,2′-bipyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Reference of 4-Amino-2-picolineOn October 24, 2019 ,《Development of Chemical Entities Endowed with Potent Fast-Killing Properties against Plasmodium falciparum Malaria Parasites》 was published in Journal of Medicinal Chemistry. The article was written by Matralis, Alexios N.; Malik, Adnan; Penzo, Maria; Moreno, Inmaculada; Almela, Maria J.; Camino, Isabel; Crespo, Benigno; Saadeddin, Anas; Ghidelli-Disse, Sonja; Rueda, Lourdes; Calderon, Felix; Osborne, Simon A.; Drewes, Gerard; Boesche, Markus; Fernandez-Alvaro, Elena; Martin Hernando, Jose Ignacio; Baker, David A.. The article contains the following contents:

One of the attractive properties of artemisinins is their extremely fast-killing capability, quickly relieving malaria symptoms. Nevertheless, the unique benefits of these medicines are now compromised by the prolonged parasite clearance times and the increasing frequency of treatment failures, attributed to the increased tolerance of Plasmodium falciparum to artemisinin. This emerging artemisinin resistance threatens to undermine the effectiveness of antimalarial combination therapies. Herein, we describe the medicinal chem. efforts focused on a cGMP-dependent protein kinase (PKG) inhibitor scaffold, leading to the identification of novel chem. entities with very potent, similar to artemisinins, fast-killing potency against asexual blood stages that cause disease, and activity against gametocyte activation that is required for transmission. Furthermore, we confirm that selective PKG inhibitors have a slow speed of kill, while chemoproteomic anal. suggests for the first time serine/arginine protein kinase 2 (SRPK2) targeting as a novel strategy for developing antimalarial compounds with extremely fast-killing properties. After reading the article, we found that the author used 4-Amino-2-picoline(cas: 18437-58-6Reference of 4-Amino-2-picoline)

4-Amino-2-picoline(cas: 18437-58-6) belongs to anime. Many important products require amines as part of their syntheses. Methylamine is utilized in the production of the analgesic meperidine (trade name Demerol) and the photographic developer Metol (trademark), and dimethylamine is used in the synthesis of the antihistamine diphenhydramine (trade name Benadryl), the solvent dimethylformamide (DMF), and the rocket propellant 1,1-dimethylhydrazine. The synthesis of the insect repellent N,N-diethyl-m-toluamide (DEET) incorporates diethylamine while that of the synthetic fibre Kevlar requires aromatic amines.Reference of 4-Amino-2-picoline

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Formula: C5H5BrN2On March 20, 2020, Li, Jianqing; Smith, Daniel; Krishnananthan, Subramaniam; Mathur, Arvind published an article in Organic Process Research & Development. The article was 《A Practical Synthesis of the TGFβRI Inhibitor N-(4-(3-(6-(Difluoromethyl)pyridin-2-yl)-1H-pyrrolo[3,2-b]pyridin-2-yl)pyridin-2-yl)acetamide via One-pot Sequential Sonogashira and Cacchi Reactions Catalyzed by Pd(OAc)2/BINAP》. The article mentions the following:

N-(4-(3-(6-(Difluoromethyl)pyridin-2-yl)-1H-pyrrolo[3,2-b]pyridin-2-yl)pyridin-2-yl)acetamide is a potent inhibitor of TGFβRI kinase that provides durable antitumor activity when combined with an anti-PD-1 antibody. In order to conduct a full range of preclin. studies, over 150 g of high quality material were required. The original discovery route through a step-wise, copper-mediated Sonogashira reaction, trifluoroacetamide formation and Cacchi reaction suffered from scale-up issues, mainly associated with tedious chromatog. purification of intermediates. This communication describes a chromatog.-free, one-pot synthesis of tittle compound via sequential Sonogashira and Cacchi reactions promoted by the superior catalyst Pd(OAc)2/BINAP, which was discovered by catalyst screening. In the experiment, the researchers used many compounds, for example, 2-Bromopyridin-3-amine(cas: 39856-58-1Formula: C5H5BrN2)

2-Bromopyridin-3-amine(cas: 39856-58-1) belongs to anime.Typically the presence of an amine functional group is deduced by a combination of techniques, including mass spectrometry as well as NMR and IR spectroscopies. 1H NMR signals for amines disappear upon treatment of the sample with D2O. In their infrared spectrum primary amines exhibit two N-H bands, whereas secondary amines exhibit only one.Formula: C5H5BrN2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem