Category: pyridine-derivatives

Gunzner-Toste, Janet; Zhao, Guiling; Bauer, Paul; Baumeister, Timm; Buckmelter, Alexandre J.; Caligiuri, Maureen; Clodfelter, Karl H.; Fu, Bang; Han, Bingsong; Ho, Yen-Ching; Kley, Nikolai; Liang, Xiaorong; Liederer, Bianca M.; Lin, Jian; Mukadam, Sophie; O’Brien, Thomas; Oh, Angela; Reynolds, Dominic J.; Sharma, Geeta; Skelton, Nicholas; Smith, Chase C.; Sodhi, Jasleen; Wang, Weiru; Wang, Zhongguo; Xiao, Yang; Yuen, Po-wai; Zak, Mark; Zhang, Lei; Zheng, Xiaozhang; Bair, Kenneth W.; Dragovich, Peter S. published the artcile< Discovery of potent and efficacious urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with reduced CYP2C9 inhibition properties>, Reference of 56622-54-9, the main research area is urea containing nicotinamide phosphoribosyltransferase inhibitor reduced CYP2C9 inhibition preparation; pharmacokinetic antitumor activity urea containing benzenesulfonamide.

Potent, reversible inhibition of the cytochrome P 450 CYP2C9 isoform was observed in a series of urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors. This unwanted property was successfully removed from the described inhibitors through a combination of structure-based design and medicinal chem. activities. An optimized compound, I, which did not inhibit CYP2C9 exhibited potent anti-NAMPT activity (BC NAMPT IC50 = 3 nM; A2780 antiproliferative IC50 = 70 nM), good mouse PK properties, and was efficacious in an A2780 mouse xenograft model. The crystal structure of this compound in complex with the NAMPT protein is also described.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 56622-54-9 belongs to class pyridine-derivatives, and the molecular formula is C7H10N2, Reference of 56622-54-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Evjen, Sigvart; Loege, Oda Siebke; Fiksdahl, Anne; Knuutila, Hanna K. published the artcile< Aminoalkyl-Functionalized Pyridines as High Cyclic Capacity CO2 Absorbents>, Computed Properties of 3731-53-1, the main research area is aminoalkyl functionalized pyridines high cyclic capacity carbon dioxide absorbent.

Recent years have witnessed a growing academic interest in the development of new CO2 capture solvents to reduce the capture costs. This study focused on nine picolylamines (three com. and six synthesized) and one imidazole-amine, most of which have not previously been reported as amine absorbents. The solvent performance was evaluated by measuring the absorption capacity, desorption tendency, and pKa. Several of the amines demonstrated CO2 cyclic capacity significantly higher than that of 30 wt % MEA due to very lean CO2 loadings, driven by low amine pKa. The lean loadings can potentially mitigate solvent degradation At the same time, absorption rates comparable to 30 wt % MEA were obtained for 3 M picolylamines. The results demonstrate the promising nature of picolylamines and derivatives for CO2 capture.

Energy & Fuels published new progress about Absorbents. 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Computed Properties of 3731-53-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Hajos, G.; Riedl, Z. published the artcile< Product class 5: azaindolizines with two nitrogen atoms in the five-membered ring>, Synthetic Route of 22280-62-2, the main research area is review azaindolizine preparation.

A review of preparation of azaindolizines with two nitrogen atoms in the five-membered ring. Covered reactions include ring-closure, substituent modification, substitution reactions, and other miscellaneous methods.

Science of Synthesis published new progress about Cyclization. 22280-62-2 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Synthetic Route of 22280-62-2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Rutgeerts, Laurens A. J.; Soultan, Al Halifa; Subramani, Ramesh; Toprakhisar, Burak; Ramon, Herman; Paderes, Monissa C.; De Borggraeve, Wim M.; Patterson, Jennifer published the artcile< Robust scalable synthesis of a bis-urea derivative forming thixotropic and cytocompatible supramolecular hydrogels>, Reference of 3731-53-1, the main research area is bis urea derivative nanofiber supramol hydrogel gelator cytocompatibility.

Synthetic hydrogels address a need for affordable, industrially scalable scaffolds for tissue engineering. Herein, a novel low mol. weight gelator is reported that forms self-healing supramol. hydrogels. Its robust synthesis can be performed in a solvent-free manner using ball milling. Strikingly, encapsulated cells spread and proliferate without specific cell adhesion ligands in the nanofibrous material.

Chemical Communications (Cambridge, United Kingdom) published new progress about Biocompatibility. 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Reference of 3731-53-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Bej, Raju; Ghosh, Suhrit published the artcile< Glutathione Triggered Cascade Degradation of an Amphiphilic Poly(disulfide)-Drug Conjugate and Targeted Release>, Recommanded Product: 1,2-Di(pyridin-2-yl)disulfane, the main research area is glutathione cascade amphiphile polydisulfide drug conjugate targeting.

A bioreducible poly(disulfide)-derived amphiphilic block copolymer-drug conjugate (loading content 31%) was synthesized by post-polymerization modification. It shows redox-responsive polymersome assembly in water with aggregation induced emission property arising from the appended Camptothecin (CPT) drug. Glutathione (GSH), a tripeptide overexpressed in cancer cells, triggers a cascade reaction resulting in simultaneous degradation of the polymer backbone (consisting of disulfide linkage) and the release of the pendant drug. The cascade reaction involves GSH trigger cleavage of the backbone disulfide bond producing free thiol followed by its intrachain nucleophilic attack to the adjacent carbonate group that links the appended drug mol. The polymeric pro-drug exhibits killing efficiency to a cancer cell with remarkably low IC50 value of 3.1μg/mL (based on the CPT concentration) while it shows negligible toxicity to a normal cell up to polymer concentration 300μg/mL.

Bioconjugate Chemistry published new progress about Aggregation-induced emission. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Recommanded Product: 1,2-Di(pyridin-2-yl)disulfane.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Iwaki, Kentaro; Maruno, Koki; Nagata, Osamu; Shibata, Norio published the artcile< Ethynyl-SF4-Pyridines: Reagents for SF4-Alkynylation to Carbonyl Compounds>, HPLC of Formula: 350-03-8, the main research area is propargylic alc tetrafluorosulfanyl pyridinyl preparation; ethynyl tetrafluoro sulfanyl pyridine preparation carbonyl compound tetrafluorosulfanyl alkynation.

The first synthesis of (ethynyl-trans-tetrafluoro-λ6-sulfanyl)pyridines I (R = H, F) and their use as versatile reagents for the first direct SF4-alkynation to carbonyl compounds R1C(O)Ar (R1 = H, Me, Ph, CF3, pyridin-2-yl; Ar = Ph, 2-methylphenyl, pyridin-3-yl, etc.) were reported. The addition reaction of t-ethynyl-SF4-pyridines I to the carbonyl group in the presence of MeLi smoothly afforded pyridine-SF4-propargylic secondary alcs. II nd tertiary alcs., e.g., III in high yields.

Journal of Organic Chemistry published new progress about Alcohols, propargyl Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 350-03-8 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO, HPLC of Formula: 350-03-8.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Talik, Tadeusz; Talik, Zofia published the artcile< Nitraminopyridines. II. Reactions of nitraminomethylpyridines with phosphorus halides>, Electric Literature of 22280-62-2, the main research area is nitramino pyridines; pyridines nitramino.

Reactions of 2-(nitramino)pyridines and 4-(nitramino)pyridines with PCl3, PCl5, PBr3, PBr5, and PI3 were studied. The nitramino group was easily exchanged for Cl, Br, or iodine. A series of chloro-, bromo-, and iodopicolines was prepared The following pyridine homologs were used as the starting material: 2-(nitramino)-3-methylpyridine (I), 2-(nitramino)-4-methylpyridine (II), 2-(nitramino)-5-methylpyridine (III), 2-(nitramino)-6-methylpyridine (IV), 4-(nitramino)-3-methylpyridine (V), 4-(nitramino)-2-methylpyridine (VI), 4-(nitramino)-2,6-dimethylpyridine (VII), and 3-(nitramino)-2,6-dimethylpyridine (VIII). The reactions were carried out in CHCl3 with 0.5 mole excess phosphorous halide at the boiling temperature Thus, a suspension of 0.01 mole nitraminomethylpyridine in 10 ml. CHCl3 was treated, under cooling, with 2.1 g. PCl3 then refluxed 1 hr., concentrated in vacuo, decomposed with ice, neutralized with NaHCO3 and steam distilled When extracted with Et2O, and the extract worked up, the distillate gave a halopicoline. The following compounds were reported (substrate, phosphones halide, product, m.p., b.p., and % yield given): I, PCl3, 2-chloro-3-methylpyridine, -, 193°, 24.1, and 2-chloro-5-nitro-3-methylpyridine (IX) 48°, -, 11.5; II, PCl3, 2-chloro-4-methylpyridine (X), -, 194°, 72.3; III, PCl3, 2-chloro-5-methylpyridine (XI), -, 86-7°/15 mm., 60.2; IV, PCl3, 2-chloro-5-nitro-6-methylpyridine (XII), 52°, -, 11.7, and 2-amino-3-nitro-6-methylpyridine (XIII), 141°, -, 6.7, and 2-amino-5-nitro-6methylpyridine, 188°, -, 13.3; V, PCl3, 4-chloro-3-methylpyridine (XIV), -, 164°, 60.2; VI, PCl3, 4-chloro-2-methylpyridine (XV), -, 162°, 72.3; VII, PCl3, 4-chloro-2,6-dimethylpyridine (XVI), -, 177°, 86.5; I, PCl5, IX, 47°, -, 26.6, and 2-amino-5-nitro-3-methylpyridine, 254°, -, 60.2; II, PCl5, X, -, 194°, 60.2; III, PCl5, XI, -, 87°/15 mm., 56.2; IV, PCl5, XII, 52°, -, 41.2, and XIII, 141°, -, 46.7; V, PCl5, XIV, -, 164°, 84.3; VI, PCl5, XV, -, 162°, 84.3; VII, PCl5, XVI, -, 177°, 86.5; I, PBr3, 2-bromo-3-methylpyridine (XVII), -, 209°, 48.5; II, PBr3, 2-bromo-4-methylpyridine (XVIII), -, 213°, 63.6, III, PBr3, 2-bromo-5-methylpyridine (XIX), 48°, -, 62.3; IV, PBr3, 2-bromo-5-nitro-6-methylpyridine (XX), 69°, -, 32.8, and 2-amino-3-nitro-6-methylpyridine (XXI), 141°, -, 20, and 2-amino-5-nitro-6-methylpyridine (XXII), 188°, -, 40; V, PBr3, PBr3, 4-bromo-3-methylpyridine (XXIII), -, 76°/15 mm., 77.1; VI, PBr3, 4-bromo-2-methylpyridine (XXIV), -, 181°, 62.3; VII, PBr3, 4-bromo-2,6-dimethylpyridine (XXV), -, 193°, 49.4; I, PBr5, XVII, -, 209°, 71.2; II, PBr5, XVIII, -, 212°, 62.3; III, PBr5, XIX, 48°, -, 62.3; IV, PBr5, XX, 69°, -, 9.4, and XXI, 141°, -, 33.3, and XXII, 188°, -, 40.0; V, PBr5, XXIII, -, 76°/15 mm., 44.5; VI, PBr5, XXIV, -, 181°, 44.5; VII, PBr5, XXV, -, 193°, 49.4; I, PI3, 2-iodo-3-methylpyridine, -, 105°, 27; II, PI3, 2-iodo-4-methylpyridine, -, 112°, 65; III, PI3, 2-iodo-5-methylpyridine, 52°, -, 69.9; V, PI3, 4-iodo-3-methylpyridine, 46°, -, 55.9; VI, PI3, 4-iodo-2-methylpyridine, 42°, -, 83.6; VII, PI3, 4-iodo-2,6-dimethylpyridine, 99°, -, 65.7. VIII did not react with phosphorus halides. Under the conditions employed, decomposition of VIII and formation of 3-amino-2,6-dimethylpyridine was observed.

Roczniki Chemii published new progress about Group 15 element halides, phosphorus halides Role: RCT (Reactant), RACT (Reactant or Reagent). 22280-62-2 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Electric Literature of 22280-62-2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Li, Xiaolan; Zhang, Xiuqi; Zhang, Fukuan; Luo, Xuzhong; Luo, Haiqing published the artcile< Construction of Pyridine Ring Systems by Mn(OAc)2-Promoted Formal Dehydrative Dehydroaromatizing [4+2] Cycloaddition of Enamides with Maleimides>, Product Details of C7H7NO, the main research area is pyrrolopyridine preparation; enamide maleimide formal dehydrative dehydroaromatizing cycloaddition manganese acetate promoted.

A Mn(OAc)2-promoted formal dehydrative dehydroaromatizing [4+2] cycloaddition of enamides with maleimides for the construction of pyridine rings to access the diverse synthetically valuable pyrrolo[3,4-c]-pyridine derivatives I [R = Ph, 4-FC6H4, 2-naphthyl, etc.; R1 = Me, Et, Bn, etc.] was reported. This protocol allowed two C-C bond formation for the assembly of pyridine derivatives from enamides synthesizable in two steps and inexpensive maleimides, which exhibited broad substrate scope and good functional group compatibility.

Advanced Synthesis & Catalysis published new progress about [4+2] Cycloaddition reaction. 350-03-8 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO, Product Details of C7H7NO.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Chen, Siyuan; Yang, Shanxiu; Wang, Hao; Niu, Yanning; Zhang, Zhang; Qian, Bo published the artcile< Continuous Flow Microreactor Promoted the Catalytic N -Oxidation Reaction of Pyridine Derivatives>, Reference of 93-60-7, the main research area is pyridine derivative catalytic oxidation continuous flow microreactor.

A simple continuous flow microreactor was successfully constructed for the N-oxidation of pyridine. The continuous flow microreactor used titanium silicalite (TS-1) in a packed-bed microreactor and H2O2 (in methanol as solvent) as the catalytic oxidation system for the formation of various pyridine N-oxides in up to 99% yields. This process is a safer, greener, and more highly efficiency process than using a batch reactor. The device was used for over 800 h of continuous operation with the catalyst maintaining great activity thus providing great potential for large-scale production

Synthesis published new progress about Flow reactors. 93-60-7 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO2, Reference of 93-60-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zurlinden, Todd J.; Saili, Katerine S.; Rush, Nathaniel; Kothiya, Parth; Judson, Richard S.; Houck, Keith A.; Hunter, E. Sidney; Baker, Nancy C.; Palmer, Jessica A.; Thomas, Russell S.; Knudsen, Thomas B. published the artcile< Profiling the ToxCast library with a pluripotent human (H9) stem cell line-based biomarker assay for developmental toxicity>, SDS of cas: 3811-73-2, the main research area is toxcast library pluripotent human stem cell line development toxicity; developmental toxicity; embryonic stem cells; predictive toxicology.

The Stemina devTOX quickPredict platform is a human pluripotent stem cell-based assay that predicts the developmental toxicity potential based on changes in cellular metabolism following chem. exposure. Using this assay, we screened 1065 ToxCast phase I and II chems. in single-concentration or concentration-response for the targeted biomarker (ratio of ornithine to cystine secreted or consumed from the media). The dataset from the Stemina (STM) assay is annotated in the ToxCast portfolio as STM. Major findings from the anal. of ToxCast_STM dataset include (1) 19% of 1065 chems. yielded a prediction of developmental toxicity, (2) assay performance reached 79%-82% accuracy with high specificity (> 84%) but modest sensitivity (< 67%) when compared with in vivo animal models of human prenatal developmental toxicity, (3) sensitivity improved as more stringent weights of evidence requirements were applied to the animal studies, and (4) statistical anal. of the most potent chem. hits on specific biochem. targets in ToxCast revealed pos. and neg. associations with the STM response, providing insights into the mechanistic underpinnings of the targeted endpoint and its biol. domain. The results of this study will be useful to improving our ability to predict in vivo developmental toxicants based on in vitro data and in silico models. Toxicological Sciences published new progress about Analysis (toxicol.). 3811-73-2 belongs to class pyridine-derivatives, and the molecular formula is C5H4NNaOS, SDS of cas: 3811-73-2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem