Month: December 2022

Brouwer, Chad published the artcileDevelopment of N-Methyl-(2-arylquinolin-4-yl)oxypropanamides as Leads to PET Radioligands for Translocator Protein (18 kDa), Safety of 2-Bromopyridin-3-amine, the publication is Journal of Medicinal Chemistry (2014), 57(14), 6240-6251, database is CAplus and MEDLINE.

Translocator protein (18 kDa), known as TSPO, is a recognized biomarker of neuroinflammation. Radioligands with PET accurately quantify TSPO in neuroinflammatory conditions. However, the existence of three human TSPO genotypes that show differential affinity to almost all useful TSPO PET radioligands hampers such studies. There is an unmet need for genotype-insensitive, high-affinity, and moderately lipophilic TSPO ligands that may serve as leads for PET radioligand development. To address this need, we varied the known high-affinity TSPO ligand (l)-N,N-diethyl-2-methyl-3-(2-phenylquinolin-4-yl)propanamide in its aryl scaffold, side chain tether, and pendant substituted amido group while retaining an N-Me group as a site for labeling with carbon-11. From this effort, oxygen-tethered N-methyl-aryloxypropanamides emerged as new high-affinity TSPO ligands with attenuated lipophilicity, including one example with attractive properties for PET radioligand development, namely N-methyl-N-phenyl-2-{[2-(pyridin-2-yl)quinolin-4-yl]oxy}propanamide (22a; rat K_i = 0.10 nM; human TSPO genotypes K_i = 1.4 nM; clogD = 4.18).

Journal of Medicinal Chemistry published new progress about 39856-58-1. 39856-58-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Bromide,Amine, name is 2-Bromopyridin-3-amine, and the molecular formula is C5H5BrN2, Safety of 2-Bromopyridin-3-amine.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Baker, Paul K. published the artcileThe synthesis of the first examples of water-soluble seven-coordinate complexes of tungsten(II), Safety of Pyridine-3-sulfonic acid, the publication is Journal of the Chemical Society, Dalton Transactions: Inorganic Chemistry (1995), 1525-6, database is CAplus.

Reaction of the seven-coordinate complex [WI₂(CO)₃(NCMe)₂] with two equivalent of 4-HO₂CC₅H₄N in MeOH at room temperature gave the bis(pyridine-4-carboxylic acid) complex [WI₂(CO)₃(4-HO₂CC₅H₄N)₂] (1) in good yield, which, upon treatment with two equivalent of NaOH in EtOH, afforded the completely water soluble complex [WI₂(CO)₃(4-NaO₂CC₅H₄N)₂] (2) in good yield; reaction of the latter with an equimolar amount of 3-NaO₃SC₅H₄N yielded [WI₂(CO)₃(4-NaO₂CC₅H₄N)(3-NaO₃SC₅H₄N)], which represents the 1st room-temperature ligand-substitution reaction in H₂O of a metal carbonyl complex.

Journal of the Chemical Society, Dalton Transactions: Inorganic Chemistry published new progress about 636-73-7. 636-73-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Sulfonic acid, name is Pyridine-3-sulfonic acid, and the molecular formula is C5H5NO3S, Safety of Pyridine-3-sulfonic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Roessler, Simon L. published the artcilePyridyl Radical Cation for C-H Amination of Arenes, Product Details of C6H5F4NO3S, the publication is Angewandte Chemie, International Edition (2019), 58(2), 526-531, database is CAplus and MEDLINE.

Electron-transfer photocatalysis provides access to the elusive and unprecedented N-pyridyl radical cation from selected N-substituted pyridinium reagents. The resulting C(sp²)-H functionalization of (hetero)arenes furnishes versatile intermediates for the development of valuable aminated aryl scaffolds. Mechanistic studies that include the first spectroscopic evidence of a spin-trapped N-pyridyl radical adduct implicate SET-triggered, pseudo-mesolytic cleavage of the N-X pyridinium reagents mediated by visible light.

Angewandte Chemie, International Edition published new progress about 107263-95-6. 107263-95-6 belongs to pyridine-derivatives, auxiliary class Fluorination reagent, name is 1-Fluoropyridiniumtriflate, and the molecular formula is C6H5F4NO3S, Product Details of C6H5F4NO3S.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Naskar, Gouranga published the artcileLigand-Enabled [3+2] Annulation of Aromatic Acids with Maleimides by C(sp³)-H and C(sp²)-H Bond Activation, Safety of Pyridine-3-sulfonic acid, the publication is Chemistry – A European Journal (2022), 28(39), e202200778, database is CAplus and MEDLINE.

Synthesis of tricyclic heterocyclic mols. I [R = 5-F, 5-Me, 5-CF₃, etc.; R¹ = Me, Et, Bn, etc.] with a free carboxylic group in a high atom- and step-economical manner via palladium-catalyzed [3+2] annulation of substituted benzoic acids with maleimides was described. The reaction proceeded via a dual C-H bond activation such as C(sp³)-H at the benzylic position and C(sp²)-H bond activation at the meta position of substituted aromatics An external ligand (MPAA) was crucial for the success of present protocol. Further, the decarboxylation and esterification of the free carboxylic acid group of observed products were carried out.

Chemistry – A European Journal published new progress about 636-73-7. 636-73-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Sulfonic acid, name is Pyridine-3-sulfonic acid, and the molecular formula is C5H5NO3S, Safety of Pyridine-3-sulfonic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Upadhyay, Nitinkumar Satyadev published the artcileRhodium-Catalyzed Regioselective Synthesis of Isoindolium Salts from 2-Arylpyridines and Alkenes in Aqueous Medium under Oxygen, Recommanded Product: 5-Methyl-2-(p-tolyl)pyridine, the publication is Advanced Synthesis & Catalysis (2016), 358(21), 3381-3386, database is CAplus.

A highly regioselective synthesis of pyrido[2,1-a]isoindolium salts, e.g., I (X-rays single crystal structure shown), from 2-arylpyridines and two equivalent of electron-deficient alkenes catalyzed by rhodium is demonstrated. The reaction was carried out in aqueous medium at 110 °C using inexpensive oxygen as oxidant. Reverse aza-Michael addition of the isoindolium salt occurs when the salt was treated with base to give a β-disubstituted alkene product. A reaction mechanism involving an ortho C-H olefination of 2-arylpyridine by alkene, intramol. aza-Michael addition, deprotonation at the β-carbon of the alkene fragment followed by another Michael addition to give the final product is proposed.

Advanced Synthesis & Catalysis published new progress about 85237-71-4. 85237-71-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene, name is 5-Methyl-2-(p-tolyl)pyridine, and the molecular formula is C9H8BNO2, Recommanded Product: 5-Methyl-2-(p-tolyl)pyridine.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Kolman, Viktor published the artcilePolysubstituted 4,6-bis(hetero)arylpyrimidines as dual inhibitors of nitric oxide and prostaglandin E₂ production, HPLC of Formula: 197958-29-5, the publication is Nitric Oxide (2017), 53-57, database is CAplus and MEDLINE.

As a part of our extensive structure-activity relationship study of anti-inflammatory heterocycles, a novel series of 67 polysubstituted 2-aminopyrimidines was prepared bearing one (at the C-4 position of the pyrimidine ring) or two (in the C-4 and C-6 positions) (hetero)aryl substituents attached directly through the C-C bond. The key synthetic steps involved either Suzuki-Miyaura or Stille cross-coupling reactions carried out on easily available 4,6-dichloropyrimidines. All prepared compounds, except one, were able to inhibit immune-activated production of nitric oxide (NO) significantly. Moreover, several compounds were found to be low micromolar dual inhibitors of NO and prostaglandin E₂ (PGE₂) production Although the exact mode of action of the prepared compounds remains to be elucidated, non-toxic dual inhibitors of NO and PGE₂ production may have great therapeutic benefit in treatment of various inflammation diseases and deserve further preclin. evaluation.

Nitric Oxide published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, HPLC of Formula: 197958-29-5.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Matsuura, Rei published the artcilePalladium(II)-catalyzed γ-selective hydroarylation of alkenyl carbonyl compounds with arylboronic acids, Application of (1-(tert-Butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)boronic acid, the publication is Chemical Science (2018), 9(44), 8363-8368, database is CAplus and MEDLINE.

A catalytic γ-selective syn-hydroarylation of alkenyl carbonyl compounds using arylboronic acids was developed using a substrate directivity approach with a palladium(II) catalyst. This method tolerated a wide range of functionalized (hetero)arylboronic acids and a variety of substitution patterns on the alkene. Preliminary mechanistic studies suggested that transmetalation is rate-limiting.

Chemical Science published new progress about 844501-00-4. 844501-00-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Amide,Boronic Acids,Boronic acid and ester, name is (1-(tert-Butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)boronic acid, and the molecular formula is C10H18BNO4, Application of (1-(tert-Butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Ceccarelli, Simona M. published the artcileRational design, synthesis, and structure-activity relationship of benzoxazolones: new potent mGlu5 receptor antagonists based on the fenobam structure, Safety of 4-Amino-2-picoline, the publication is Bioorganic & Medicinal Chemistry Letters (2007), 17(5), 1302-1306, database is CAplus and MEDLINE.

A class of potent and stable mGlu5 receptor antagonists was developed by combining information from a high-throughput screening campaign with the structure of the known anxiolytic fenobam. Representative compounds I from this class show favorable pharmacokinetic properties and are active in an in vivo model of anxiety.

Bioorganic & Medicinal Chemistry Letters published new progress about 18437-58-6. 18437-58-6 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 4-Amino-2-picoline, and the molecular formula is C6H8N2, Safety of 4-Amino-2-picoline.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Lee, Kum-Tatt published the artcileDetermination of serum iron and zinc by atomic absorption spectroscopy, Safety of 2-((2-(Pyridin-2-yl)hydrazono)methyl)pyridine, the publication is Mikrochimica Acta (1974), 65-72, database is CAplus and MEDLINE.

An improved, rapid, and precise method was developed for the simultaneous determination of Fe and Zn in serum by at. absorption spectroscopy. The new procedure avoided the clogging of the burner head and possible contamination from Hb Fe, which could occur in other at. absorption methods; it also yielded accurate data when the Fe concentration was <200 μg/100 ml serum, as well as in the higher ranges. The method dependend upon the efficient complexing of serum Fe and Zn with pyridine-2-aldehyde 2-pyridylhydrazone. Although these metal chelates were practically insoluble in aqueous media, by shifting the pH to the alk. side with KOH, they could be extracted quant. into an organic solvent, such as amyl alc. This organic extract could then be aspirated into the air-C2H2 flame of the spectrometer. Even in the lower ranges, the procedure yielded good reproducibility. The method can also be applied to urine samples.

Mikrochimica Acta published new progress about 2215-33-0. 2215-33-0 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 2-((2-(Pyridin-2-yl)hydrazono)methyl)pyridine, and the molecular formula is C11H10N4, Safety of 2-((2-(Pyridin-2-yl)hydrazono)methyl)pyridine.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Fatemi, Mohammad H. published the artcileIn silico cytotoxicity estimation of ionic liquids based on their two- and three-dimensional structural descriptors, COA of Formula: C7H7ClN2, the publication is Monatshefte fuer Chemie (2011), 142(11), 1111-1119, database is CAplus.

The cytotoxicity of a series of ionic liquids containing ammonium, pyrrolidinium, imidazolium, pyridinium, and piperidinium cations against leukemia rat cell line IPC-81 was estimated from their structural parameters using quant. structure-activity relationship methodol. Linear and nonlinear models were developed using genetic algorithm multiple linear regression and multilayer perceptron neural network approaches. Robustness and reliability of the constructed models were evaluated by internal, external, and Y-randomization procedures. Furthermore, the chem. applicability domain was determined via a leverage approach for each model. The results of this study revealed that the contribution of structural characteristics of the anionic parts of the studied ILs were fewer than of the cationic parts.

Monatshefte fuer Chemie published new progress about 17281-59-3. 17281-59-3 belongs to pyridine-derivatives, auxiliary class Pyridine,Nitrile,Salt, name is 1-(Cyanomethyl)pyridin-1-ium chloride, and the molecular formula is C7H7ClN2, COA of Formula: C7H7ClN2.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem