Day: November 30, 2022

Puvvala, Srinu published the artcileOne-Pot Synthesis of 7-chloro-2-arylthieno[3,2-b]pyridin-3-ols and Their Derivatization to the Corresponding Arylamino, Arylthio, and Aryloxy Derivatives, Recommanded Product: Methyl 4-chloropicolinate, the main research area is chloroarylthienopyridinol arylamino arylthio aryloxy derivative preparation.

A simple and efficient domino reaction for synthesis of 7-chloro-2-arylthieno[3,2-b]pyridin-3-ols followed by derivatization into their corresponding aminoaryl, aryloxy , and thioaryloxy derivatives is presented. The synthesis includes thioalkylation on 3-position of Me 4-chloropicolinate followed by in situ cyclization to give 7-chloro-2-arylthieno[3,2-b]pyridin-3-ols. The substitution of the chloro group with amines, phenols and thiophenols afforded the corresponding derivatives

Journal of Heterocyclic Chemistry published new progress about Aromatic amines Role: SPN (Synthetic Preparation), PREP (Preparation). 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, Recommanded Product: Methyl 4-chloropicolinate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Yu, Chengzhi published the artcileSamarium(0) and 1,1′-Dioctyl-4,4′-Bipyridinium Dibromide: A Novel Electron-Transfer System for the Chemoselective Reduction of Aromatic Nitro Groups, Application In Synthesis of 36437-30-6, the main research area is reduction aromatic nitro group samarium bipyridinium dibromide catalyst; electron transfer catalyst dioctylbipyridinium dibromide; amine aromatic preparation.

A mild and efficient electron-transfer method was developed for the chemoselective reduction of aromatic nitro groups using samarium(0) metal in the presence of a catalytic amount of 1,1′-dioctyl-4,4′-bipyridinium dibromide. This method was found to give the product aromatic amine in 79-99% yield with selectivity over a number of other functional and protecting groups such as alkene, azide, benzyl ether, nitrile, amide, halide, p-toluenesulfonamide, t-Boc, tert-butyldiphenylsilyl ether, and aliphatic nitro groups. Our results also indicate that samarium(0) plays an important role in the reduction process and that 1,1′-dioctyl-4,4′-bipyridinium dibromide acts as an electron-transfer catalyst and is essential in the activation of samarium(0) metal. The major active reducing agent responsible for the reduction is believed to be the radical cation species formed from 1,1′-dioctyl-4,4′-bipyridinium dibromide.

Journal of Organic Chemistry published new progress about Aromatic amines Role: SPN (Synthetic Preparation), PREP (Preparation). 36437-30-6 belongs to class pyridine-derivatives, name is 1,1-Di-n-octyl-4,4-bipyridinium Dibromide, and the molecular formula is C26H42Br2N2, Application In Synthesis of 36437-30-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Li, Dingzhong published the artcileIndustrial Cunninghamia lanceolata carbon supported FeO(OH) nanoparticles-catalyzed hydrogenation of nitroarenes, Application of 2-Chloro-4-methylpyridin-3-amine, the main research area is cunninghamia lanceolata carbon support iron hydroxide oxide catalyst preparation; nitroarene iron hydroxide oxide catalyst hydrogenation; aryl amine green preparation.

An industrial Cunninghamia lanceolata carbon supported FeO(OH) nanoparticles process for the synthesis of aryl amines with good yields via hydrogenation of nitroarenes was reported. Nine key anti-cancer drug intermediates were successfully achieved with protocol. And Osimertinib intermediate could be smoothly synthesized at a 2.67 kg-scale with >99.5% HPLC purity. This protocol featured cheap carbon source, highly catalytic activity, simple operation, kilogram-scalable and recyclable catalysts (eight times without observable losing activity).

Catalysis Communications published new progress about Aromatic amines Role: SPN (Synthetic Preparation), PREP (Preparation). 133627-45-9 belongs to class pyridine-derivatives, name is 2-Chloro-4-methylpyridin-3-amine, and the molecular formula is C6H7ClN2, Application of 2-Chloro-4-methylpyridin-3-amine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, Dongping published the artcileDimeric Manganese-Catalyzed Hydroarylation and Hydroalkenylation of Unsaturated Amides, COA of Formula: C8H8BNO2, the main research area is aralkyl alkenyl amide regioselective chemoselective preparation; gamma delta lactam regioselective preparation; dimanganese catalyst regioselective chemoselective arylation alkenylation unsaturated amide; regioselective chlorocyclization phenylsulfenocyclization unsaturated amide; alkene; alkenylation; arylation; homogeneous catalysis; manganese.

In the presence of the manganese(I) dimer Mn2Br2(CO)8, either K2CO3 or CsF, and ethanol, α,β-unsaturated amides underwent chemo- and regioselective arylation and alkenylation reactions with aryl- and alkenylboronic acids to yield β-aryl amides and γ,δ-unsaturated amides. Selected γ,δ-unsaturated amides underwent chlorocyclization and phenylsulfenocyclization reactions to yield γ- and δ-lactams.

Angewandte Chemie, International Edition published new progress about Amides Role: SPN (Synthetic Preparation), PREP (Preparation) (β-aryl). 917471-30-8 belongs to class pyridine-derivatives, name is (5-(Prop-1-yn-1-yl)pyridin-3-yl)boronic acid, and the molecular formula is C8H8BNO2, COA of Formula: C8H8BNO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, Hong-Jun published the artcileEfficient N-Arylation/Dealkylation of Electron Deficient Heteroaryl Chlorides and Bicyclic Tertiary Amines under Microwave Irradiation, Name: Ethyl 6-chloropicolinate, the main research area is heteroaryl chloroethyl piperazine microwave assisted preparation; arylation dealkylation electron deficient heteroaryl chloride bicyclic tertiary amine; microwave assisted heteroaryl chloroethyl piperidine preparation.

A highly efficient procedure was developed for the microwave-assisted synthesis of N-heteroaryl-4-(2-chloroethyl)piperazines and N-heteroaryl-4-(2-chloroethyl)piperidines. Microwave irradiation of electron deficient heteroaryl chlorides with 1,4-diazabicyclo[2.2.2]octane (DABCO) at 160 °C for 15 min led to N-heteroaryl-4-(2-chloroethyl)piperazines in good to excellent yields. In a similar manner, microwave irradiation of electron deficient heteroaryl chlorides with quinuclidine at 180 °C for 15 min provided N-heteroaryl-4-(2-chloroethyl)piperidines in good to excellent yields. Extension of the method was demonstrated by the development of a one-pot, two-step microwave-assisted protocol for the synthesis of 4-(2-acetoxyethyl)-substituted N-heteroarylpiperazines and N-heteroarylpiperidines to demonstrate the production of a small library in a parallel fashion.

Journal of Combinatorial Chemistry published new progress about Aryl chlorides Role: RCT (Reactant), RACT (Reactant or Reagent) (hetero). 21190-89-6 belongs to class pyridine-derivatives, name is Ethyl 6-chloropicolinate, and the molecular formula is C8H8ClNO2, Name: Ethyl 6-chloropicolinate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Savarimuthu, Sebastian Antony published the artcileSodium Tertiary Pentoxide as a Mild and Efficient Base to Make C-C Bond between Acetylenes and Aldehydes (or) Ketones Producing Propargyl Alcohols, COA of Formula: C7H7NO2, the main research area is carbonyl compound phenylacetylene sodium tertiary pentoxide promoter green coupling; propargyl alc preparation.

This report confirmed that sodium tertiary-pentoxide was a very effective base for the nucleophilic addition of acetylenes to aldehydes and ketones in 1,4-dioxane at room temperature These mild and operationally simple procedures were working well with a variety of aromatic and heteroaromatic aldehydes and also equally working well with aliphatic, aromatic and heteroaromatic ketones. A very clean product of secondary and tertiary propargylic alcs. were obtained from 70-94% yield. This process was explored in bulk scale synthesis on selected mols. and also adapted the column free purification for most of the substrates.

ChemistrySelect published new progress about Alcohols, propargyl Role: SPN (Synthetic Preparation), PREP (Preparation). 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, COA of Formula: C7H7NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ormerod, Kiel G. published the artcileRegulation of excitation-contraction coupling at the Drosophila neuromuscular junction, Safety of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is Drosophila neuromuscular junction excitation contraction coupling; drosophila; neuromuscular junction; synapse.

The Drosophila neuromuscular system is widely used to characterize synaptic development and function. However, little is known about how specific synaptic alterations effect neuromuscular transduction and muscle contractility, which ultimately dictate behavioral output. Here we develop and use a force transducer system to characterize excitation-contraction coupling at Drosophila larval neuromuscular junctions (NMJs), examining how specific neuronal and muscle manipulations disrupt muscle contractility. Muscle contraction force increased with motoneuron stimulation frequency and duration, showing considerable plasticity between 5 and 40 Hz and saturating above 50 Hz. Endogenous recordings of fictive contractions revealed average motoneuron burst frequencies of 20-30 Hz, consistent with the system operating within this plastic range of contractility. Temperature was also a key factor in muscle contractility, as force was enhanced at lower temperatures and dramatically reduced with increasing temperatures Pharmacol. and genetic manipulations of critical components of Ca2+ regulation in both pre- and postsynaptic compartments affected the strength and time course of muscle contractions. A screen for modulators of muscle contractility led to identification and characterization of the mol. and cellular pathway by which the FMRFa peptide, TPAEDFMRFa, increases muscle performance. These findings indicate Drosophila NMJs provide a robust system to correlate synaptic dysfunction, regulation and modulation to alterations in excitation-contraction coupling. Key points : Larval muscle contraction force increases with stimulation frequency and duration, revealing substantial plasticity between 5 and 40 Hz. Fictive contraction recordings demonstrate endogenous motoneuron burst frequencies consistent with the neuromuscular system operating within the range of greatest plasticity. Genetic and pharmacol. manipulations of critical components of pre- and postsynaptic Ca2+ regulation significantly affect the strength and time course of muscle contractions. A screen for modulators of the excitation-contraction machinery identified a FMRFa peptide, TPAEDFMRFa and its associated signalling pathway, that dramatically increases muscle performance. Drosophila serves as an excellent model for dissecting components of the excitation-contraction coupling machinery.

Journal of Physiology (Oxford, United Kingdom) published new progress about Actins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Safety of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Estrada-Soto, Samuel published the artcileAntihypertensive and vasorelaxant mode of action of the ethanol-soluble extract from Tagetes lucida Cav. aerial parts and its main bioactive metabolites, Product Details of C17H18N2O6, the main research area is ethanol soluble tagetes lucida antihypertensive vasorelaxant mode bioactive metabolite; Antihypertensive; Calcium channel blockade; Coumarins; NO/cGMP system; Tagetes lucida; Vasorelaxant.

Tagetes lucida Cav. commonly known as “”yauhtli”” or “”pericoń”” is used in Mexican traditional medicine for the treatment of anxiety, depressant diseases, pain, hypertension, among others. To evaluate the antihypertensive and vasorelaxant modes of action of a crude ethanolic extract from T. lucida aerial parts and to isolate the bioactive compounds Ethanolic extract was tested in an in vivo assay in SHR rats by intragastric administration at 10 and 100 mg/kg dosages, to measure and to compare hemodynamic parameters like diastolic and systolic blood pressure and heart rate. Also, extract (3.03-1000μg/mL), fractions (3.03-1000μg/mL) and pure isolated compounds (1.75-550μM) were evaluated on isolated aortic rings contracted with noradrenaline (0.1μM) to determine their vasorelaxant effect and extract-mode of action.Ethanolic extract of T. lucida lowered systolic and diastolic blood pressure on SHR rats without heart rate modification (P > 0.05). Moreover, the extract showed concentration-dependent relaxant effect in a partially endothelium-dependent manner (P < 0.05), through NO/cGMP system activation and calcium channel blockade. 6,7,8-trimethoxycoumarin (1), 6,7-dimethoxycoumarin (2), and 7-methoxycoumarin (3) from T. lucida are the main bioactive compounds of the extract and showed significant vasorelaxant activity. Results provide evidence and endorsed the antihypertensive properties attributed to T. lucida in traditional medicine, which is produced by vasorelaxant effect mainly through multitarget NO/cGMP system activation and calcium channel blockade. Coumarin derivatives 1, 2 and 3 are the responsible of the vasorelaxant activity. Journal of Ethnopharmacology published new progress about Adrenoceptors Role: PAC (Pharmacological Activity), BIOL (Biological Study). 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Product Details of C17H18N2O6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Murphy, Rebecca A. published the artcileDirect Methoxypyridine Functionalization Approach to Magellanine-Type Lycopodium Alkaloids, Application of 2-Methoxynicotinaldehyde, the main research area is enantioselective synthesis tetracyclic core magellanine Lycopodium alkaloid; Hajos Parrish reaction enantioselective synthesis magellanine Lycopodium alkaloid; palladium catalyzed pyridine functionalization enantioselective synthesis magellanine Lycopodium alkaloid.

A concise enantioselective approach to the tetracyclic core of the magellanine-type Lycopodium alkaloids is reported. Key to this approach is the use of the Hajos-Parrish reaction to set a challenging quaternary stereocenter, thereby guiding the stereoselectivity for the remainder of the synthesis, as well as the use of a palladium-mediated direct pyridine functionalization reaction to forge the tetracyclic core.

Organic Letters published new progress about Alkaloids Role: SPN (Synthetic Preparation), PREP (Preparation) (Lycopodium). 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Application of 2-Methoxynicotinaldehyde.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mango, Katalin published the artcileCYP2B6 allelic variants and non-genetic factors influence CYP2B6 enzyme function, Related Products of pyridine-derivatives, the main research area is CYP2B6 allele genotype phenotype amoxicillin clavulanic acid cyclophosphamide.

Human CYP2B6 enzyme although constitutes relatively low proportion (1-4%) of hepatic cytochrome P 450 content, it is the major catalyst of metabolism of several clin. important drugs (efavirenz, cyclophosphamide, bupropion, methadone). High interindividual variability in CYP2B6 function, contributing to impaired drug-response and/or adverse reactions, is partly elucidated by genetic polymorphisms, whereas non-genetic factors can significantly modify the CYP2B6 phenotype. The influence of genetic and phenoconverting non-genetic factors on CYP2B6-selective activity and CYP2B6 expression was investigated in liver tissues from Caucasian subjects (N = 119). Strong association was observed between hepatic S-mephenytoin N-demethylase activity and CYP2B6 mRNA expression (P < 0.0001). In less than one third of the tissue donors, the CYP2B6 phenotype characterized by S-mephenytoin N-demethylase activity and/or CYP2B6 expression was concordant with CYP2B6 genotype, whereas in more than 35% of the subjects, an altered CYP2B6 phenotype was attributed to phenoconverting non-genetic factors (to CYP2B6-specific inhibitors and inducers, non-specific amoxicillin + clavulanic acid treatment and chronic alc. consumption, but not to the gender). Furthermore, CYP2B6 genotype-phenotype mismatch still existed in one third of tissue donors. In conclusion, identifying potential sources of CYP2B6 variability and considering both genetic variations and non-genetic factors is a pressing requirement for appropriate elucidation of CYP2B6 genotype-phenotype mismatch. Scientific Reports published new progress about Alcohols Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Related Products of pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem