Tag: M.W=200-250

Dziuganowska, Zofia A.; Slepokura, Katarzyna; Volle, Jean-Noel; Virieux, David; Pirat, Jean-Luc; Kafarski, Pawel published the artcile< Structural Analogues of Selfotel>, Recommanded Product: Methyl 3-bromo-2-pyridinecarboxylate, the main research area is phosphonate pyridinecarboxylic piperidinecarboxylic preparation phosphonylation bromopyridine hydrogenation; NMDA antagonist library phosphonate pyridinecarboxylic piperidinecarboxylic acid preparation activity; crystal structure phosphonate pyridinecarboxylic piperidinecarboxylic acid NMDA antagonist; mol structure phosphonate pyridinecarboxylic piperidinecarboxylic acid NMDA antagonist.

A small library of phosphonopiperidylcarboxylic acids, analogs of NMDA antagonist selfotel (CGS 19755), was synthesized. First, the series of aromatic esters was obtained via a palladium-catalyzed cross-coupling reaction (Hirao coupling) of dialkyl phosphites with bromopyridinecarboxylates, followed by their hydrolysis. Then, hydrogenation of the resulting phosphonopyridylcarboxylic acids over PtO2 yielded the desired phosphonopiperidylcarboxylic acids. NMR studies indicated that the hydrogenation reaction proceeds predominantly by cis addition Several compounds were obtained as monocrystal structures. Preliminary biol. studies performed on cultures of neurons suggest that the obtained compounds possess promising activity toward NMDA receptors.

Journal of Organic Chemistry published new progress about Carboxylic esters Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 53636-56-9 belongs to class pyridine-derivatives, and the molecular formula is C7H6BrNO2, Recommanded Product: Methyl 3-bromo-2-pyridinecarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Bourbeau, Matthew P.; Ashton, Kate S.; Yan, Jie; St. Jean, David J. published the artcile< Nonracemic Synthesis of GK-GKRP Disruptor AMG-3969>, Recommanded Product: tert-Butyl (5-aminopyridin-2-yl)carbamate, the main research area is AMG3969 nonracemic preparation glucokinase glucokinase regulatory protein disruptor.

A nonracemic synthesis of the glucokinase-glucokinase regulatory protein disruptor AMG-3969 (I) is reported. Key features of the synthetic approach are an asym. synthesis of the 2-alkynyl piperazine core via a base-promoted isomerization and a revised approach to the synthesis of the aminopyridinesulfonamide with an improved safety profile.

Journal of Organic Chemistry published new progress about Isomerization. 220731-04-4 belongs to class pyridine-derivatives, and the molecular formula is C10H15N3O2, Recommanded Product: tert-Butyl (5-aminopyridin-2-yl)carbamate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Iddon, Brian; Meth-Cohn, Otto; Suschitzky, Hans; Taylor, Jack A.; Wakefield, Basil J. published the artcile< Carbon-13 NMR spectra of polychloropyridines; structural assignments>, Reference of 14121-36-9, the main research area is carbon NMR chloropyridine; pyridine chloro carbon NMR.

13C NMR spectroscopy is used to distinguish between the structures of 2- and 4-substituted tetrachloropyridines. Assignments are based on comparison with pyridine, nuclear Overhauser effects, off-resonance proton decoupling, empirical chem. shift increments, and 13C-19F coupling constants

Tetrahedron Letters published new progress about NMR (nuclear magnetic resonance). 14121-36-9 belongs to class pyridine-derivatives, and the molecular formula is C5HCl4N, Reference of 14121-36-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Van der Plas, Steven E.; Kelgtermans, Hans; Mammoliti, Oscar; Menet, Christel; Tricarico, Giovanni; De Blieck, Ann; Joannesse, Caroline; De Munck, Tom; Lambin, Dominique; Cowart, Marlon; Dropsit, Sebastien; Martina, Sebastien L. X.; Gees, Maarten; Wesse, Anne-Sophie; Conrath, Katja; Andrews, Martin published the artcile< Discovery of GLPG2451, a Novel Once Daily Potentiator for the Treatment of Cystic Fibrosis>, Formula: C6H5BrN2O2, the main research area is preparation GLPG2451 analog CFTR potentiator cystic fibrosis structure.

Cystic fibrosis (CF) is a life-threatening recessive genetic disease caused by mutations in the gene encoding for the cystic fibrosis transmembrane conductance regulator (CFTR). With the discovery of Ivacaftor and Lumacaftor, it has been shown that administration of one or more small mols. can partially restore the CFTR function. Correctors are small mols. that enhance the amount of CFTR on the cell surface, while potentiators improve the gating function of the CFTR channel. Herein, the discovery and optimization of a novel potentiator series are described. Scaffold hopping, focusing on retaining the different intramol. contacts, was crucial in the whole discovery process to identify a novel series devoid of genotoxic liabilities. From this series, the clin. candidate GLPG2451 was selected based on its pharmacokinetic properties, allowing QD dosing and based on its low CYP induction potential.

Journal of Medicinal Chemistry published new progress about CFTR (cystic fibrosis transmembrane conductance regulator) Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 870997-85-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrN2O2, Formula: C6H5BrN2O2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Arya, Kritika; Kumar, Sudesh; Arya, Anand Kumar; Kumar, Mahendra published the artcile< Ionic Liquid [PyN(CH2)4SO3H][CH3PhSO3] Mediated & Promoted Eco-Friendly One-Pot Domino Synthesis of Benzothiazolopyrano/Chromenopyrimidine Derivatives>, Application In Synthesis of 21876-43-7, the main research area is benzothiazolopyranopyrimidinone preparation green chem; aldehyde aminobenzothiazole pyrone multicomponent domino heterocyclization pyridinium ionic liquid; benzothiazolochromenopyrimidinone preparation green chem; hydroxycoumarin aldehyde aminobenzothiazole multicomponent domino heterocyclization pyridinium ionic liquid; pyridinium toluenesulfonic acid ionic liquid catalyst preparation.

The pyridinium based p-toluenesulfonic acid functionalized [Py(CH2)4SO3H][CH3PhSO3] ionic liquid has been employed as eco-friendly solvent cum promoter for the multicomponent domino heterocyclization of substituted 2-aminobenzothiazoles I (R1 = H, Me; R2 = H, Me; R3 = H, Me, Br; R4 = H, Me) with 4-hydroxy-6-methyl-2-pyrone/4-hydroxycoumarin and aryl aldehydes 4-R5C6H4CHO (R5 = MeO, Cl) to produce benzothiazolo[2,3-b]pyrano [3,4-e]pyrimidin-4-ones II and benzothiazolo[2,3-b]chromeno[3,4-e]pyrimidin-6-ones III in excellent yields. The Bronsted acidic ionic liquid could be reused five-times without a significant loss of catalytic activity. The protocol proves to be efficient and facile in terms of high yields, operational simplicity, reduced reaction time and ease of recovery of the reaction medium.

Current Organocatalysis published new progress about Benzothiazoles Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 21876-43-7 belongs to class pyridine-derivatives, and the molecular formula is C9H13NO3S, Application In Synthesis of 21876-43-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Elvidge, J. A.; Zaidi, N. A. published the artcile< Heterocyclic syntheses with malonyl chloride. IX. 2-Substituted 4-chloro-6-pyrimidones from certain nitriles>, Application of C5HCl4N, the main research area is nitriles malonyl chloride; malonyl chloride nitriles; pyrimidines; pyridines.

Chloroacetonitrile with malonyl chloride yielded 2,3-dichloro-4,6-dihydroxypyridine (I) together with an unexpected product, 4-chloro-2-chloromethyl-6-pyrimidone (II). Further examples of this new synthesis of 2-substituted 4-chloro-6-pyrimidones were obtained with fluoro- and bromoacetonitrile, α-bromopropionitrile, and acetonitrile. Propio- and butyronitrile each gave a mixture of pyridine and pyrimidine product, while various other nitriles gave only the pyridine products. The expected fully substituted pyrimidone was obtained from fluoroacetonitrile and chloromalonyl chloride, and from dibromoacetonitrile with bromomalonyl chloride. Some novel halogen-transfer reactions were encountered in other cases.

Journal of the Chemical Society [Section] C: Organic published new progress about Nitriles Role: RCT (Reactant), RACT (Reactant or Reagent). 14121-36-9 belongs to class pyridine-derivatives, and the molecular formula is C5HCl4N, Application of C5HCl4N.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Hsu, Nai-Shu; Lee, Cheng-Chung; Kuo, Wen-Chih; Chang, Ya-Wen; Lo, Shin-Yi; Wang, Andrew H.-J. published the artcile< Development of a Versatile and Modular Linker for Antibody-Drug Conjugates Based on Oligonucleotide Strand Pairing>, HPLC of Formula: 2127-03-9, the main research area is linker antibody drug conjugate oligonucleotide pairing.

Linker design is crucial to the success of antibody-drug conjugates (ADCs). In this work, we developed a modular linker format for attaching mol. cargos to antibodies based on strand pairing between complementary oligonucleotides. We prepared antibody-oligonucleotide conjugates (AOCs) by attaching 18-mer oligonucleotides to an anti-HER2 antibody through thiol-maleimide chem., a method generally applicable to any Ig with interchain disulfide bridges. The hybridization of drug-bearing complementary oligonucleotides to our AOCs was rapid, stoichiometric, and sequence-specific. AOCs loaded with cytotoxic payloads were able to selectively target HER2-overexpressing cell lines such as SK-BR-3 and N87, with in vitro potencies similar to that of the marketed ADC Kadcyla (T-DM1). Our results demonstrated the potential of utilizing AOCs as a highly versatile and modular platform, where a panel of well-characterized AOCs bearing DNA, RNA, or various nucleic acid analogs, such as peptide nucleic acids, could be easily paired with any cargo of choice for a wide range of diagnostic or therapeutic applications.

Bioconjugate Chemistry published new progress about Antibody-drug conjugates. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, HPLC of Formula: 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wzgarda-Raj, Kinga; Nawrot, Martyna; Rybarczyk-Pirek, Agnieszka J.; Palusiak, Marcin published the artcile< Ionic cocrystals of dithiobispyridines: the role of I···I halogen bonds in the building of iodine frameworks and the stabilization of crystal structures>, Reference of 2127-03-9, the main research area is cocrystal; crystal structure; halogen bonding; hydrogen bonding; proton sponge; proton transfer; pyridine; quantum chemistry; salt; supramolecular chemistry.

It has been confirmed that mercaptopyridines undergo spontaneous condensation in redox reaction with iodine-forming dithiopyridines. In the solid state, these compounds are protonated at the N atoms and cocrystallize with iodine forming salt structures, namely, 2-[(pyridin-2-yl)disulfanyl]pyridinium triiodide sesquiiodine, C10H9N2S2+·I3-·1.5I2, and 4,4′-(disulfanediyl)dipyridinium pentaiodide triiodide, C10H10N2S22+·I5-·I3-. Dithiopyridine cations are packed among three-dimensional frameworks built from iodide anions and neutral iodine mols., and are linked by hydrogen, halogen and chalcogen interactions. Quantum chem. computations indicated that dithiopyridines exhibit anomalously high nitrogen basicity which qualify them as potential proton sponges.

Acta Crystallographica, Section C: Structural Chemistry published new progress about Cocrystallization. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Reference of 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Song, Jiahan; Si, Yubing; Guo, Wei; Wang, Donghai; Fu, Yongzhu published the artcile< Organosulfide-Based Deep Eutectic Electrolyte for Lithium Batteries>, Product Details of C10H8N2S2, the main research area is dipyridyl disulfide deep eutectic electrolyte lithium battery; 2,2′-dipyridyl disulfide; LiTFSI; deep eutectic electrolyte; ionic conductivity; lithium iron phosphate.

Deep eutectic electrolytes (DEEs) are a new class of electrolytes with unique properties. However, the intermol. interactions of DEEs are mostly dominated by Li···O interactions, limiting the diversity of chem. space and material constituents. Herein, we report a new class of DEEs induced by Li···N interactions between 2,2-dipyridyl disulfide (DpyDS) and lithium bis(trifluoromethanesulfonyl)imide (LiTFSI). The strong ion-dipole interaction triggers the deep eutectic phenomenon, thus liberating the Li+ from LiTFSI and endowing the DEEs with promising ionic conductivity These DEEs show admirable intrinsic safety, which cannot be ignited by flame. The DEE at the molar ratio of DpyDS_LiTFSI=4:1 (abbreviated as DEE-4:1) is electrochem. stable between 2.1 and 4.0 V vs. Li/Li+, and exhibits an ionic conductivity of 1.5×10-4 S cm-1 at 50°C. The Li/LiFePO4 half cell with DEE-4:1 can provide a reversible capacity of 130 mAh g-1 and Coulombic efficiency above 98% at 50°C.

Angewandte Chemie, International Edition published new progress about Battery capacity. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Product Details of C10H8N2S2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kalkman, Eric D.; Mormino, Michael G.; Hartwig, John F. published the artcile< Unusual Electronic Effects of Ancillary Ligands on the Perfluoroalkylation of Aryl Iodides and Bromides Mediated by Copper(I) Pentafluoroethyl Complexes of Substituted Bipyridines>, Safety of 4,4′-Dichloro-2,2′-bipyridine, the main research area is Perfluoroalkylation aryl halides Copper pentafluoroethyl complex Bipyridines LFER; kinetics Perfluoroalkylation aryl halides Copper pentafluoroethyl complex Bipyridines.

Several perfluoroalkylcopper compounds have been reported previously that serve as reagents or catalysts for the perfluoroalkylation of aryl halides. However, the relationships between the reactivity of such complexes and the electronic properties of the ancillary ligands are unknown, and such relationships are not well-known in general for copper complexes that mediate or catalyze cross coupling. We report the synthesis and characterization of a series of pentafluoroethylcopper(I) complexes ligated by bipyridine ligands possessing varied electronic properties. In contrast to the limited existing data on the reactivity of L2Cu(I)-X complexes bearing amine and pyridine-type ligands in Ullmann-type aminations with aryl halides, the reactions of aryl halides with pentafluoroethylcopper(I) complexes bearing systematically varied bipyridine ligands were faster for complexes bearing less electron-donating bipyridines than for complexes bearing more electron-donating bipyridines. Anal. of the rates of reaction and the relative populations of the neutral complexes and ionic complexes formed by these reagents in solution suggests that this effect of electronics on the reaction rate results from an unusual trend of faster oxidative addition of aryl halides to complexes containing less electron-donating ligands than to those containing more electron-donating ligands.

Journal of the American Chemical Society published new progress about Activation enthalpy. 1762-41-0 belongs to class pyridine-derivatives, and the molecular formula is C10H6Cl2N2, Safety of 4,4′-Dichloro-2,2′-bipyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem