Month: November 2022

Zeng, Jiajun published the artcileA practical access to 1,2-dicarbonyls via oxidation of alkynes catalyzed by gold(I) immobilized on MCM-41, Recommanded Product: 2-(Thiophen-2-yl)quinoxaline, the main research area is dicarbonyl preparation; alkyne oxidation MCM41 anchored diphenylphosphine gold complex; MCM41 anchored diphenylphosphine gold complex catalyst preparation.

The heterogeneous gold(I)-catalyzed oxidation of alkynes was achieved by using 2,3-dichloropyridine N-oxide as oxidant and MCM-41-anchored diphenylphosphine-gold(I) complex [MCM-41-Ph2P-AuNTf2] as the catalyst under mild and acid-free conditions, yielding diverse 1,2-dicarbonyls in good to excellent yields with easy recycling of the gold catalyst. The developed method is applicable to a wide variety of alkynes including internal or terminal alkynes, alkynyl ethers or thioethers and ynamides, and can tolerate a wide range of functional groups.

Journal of Organometallic Chemistry published new progress about Alkynes, internal Role: RCT (Reactant), RACT (Reactant or Reagent). 40353-41-1 belongs to class quinoxaline, name is 2-(Thiophen-2-yl)quinoxaline, and the molecular formula is C12H8N2S, Recommanded Product: 2-(Thiophen-2-yl)quinoxaline.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Zhang, Wei published the artcilePalladium-Catalyzed Chelation-Assisted Aromatic C-H Nitration: Regiospecific Synthesis of Nitroarenes Free from the Effect of the Orientation Rules, Related Products of quinoxaline, the main research area is arene palladium chelation assisted regiospecific ortho nitration catalyst; nitroarene preparation; aryl oxime palladium chelation assisted regiospecific ortho nitration catalyst; nitro aryl ketone preparation.

A palladium-catalyzed chelation-assisted ortho-nitration of aryl C-H bond is described. A range of azaarenes such as 2-arylquinoxalines, pyridines, quinoline, and pyrazoles were nitrated with excellent chemo- and regioselectivity. Using the O-Me oximyl group as a removable directing group, the regiospecific synthesis of a variety of o-nitro aryl ketones was achieved starting from aryl ketones via a three-step process involving the Pd-catalyzed ipso-nitration of C-H bond as a key step. Mechanistic investigations support a silver-mediated radical mechanism involving Pd(II/III) and/or Pd(II/IV) catalytic cycles under oxidizing conditions.

Journal of Organic Chemistry published new progress about Aromatic hydrocarbons Role: RCT (Reactant), RACT (Reactant or Reagent). 40353-41-1 belongs to class quinoxaline, name is 2-(Thiophen-2-yl)quinoxaline, and the molecular formula is C12H8N2S, Related Products of quinoxaline.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Petiot, Pauline published the artcilePalladium-catalyzed cross-coupling reaction of functionalized aryl- and hetero-arylbismuthanes with 2-halo(or 2-triflyl)-azines and -diazines, Recommanded Product: 2-(Thiophen-2-yl)quinoxaline, the main research area is aryl heteroarene preparation; heteroaryl halide arylbismuthane cross coupling palladium catalyst.

The palladium-catalyzed cross-coupling of highly functionalized organobismuthanes with 2-halo(or 2-triflyl)pyridines, -pyrimidines, -pyrazines, and -pyridazines is reported. The reaction tolerates numerous functional groups, including aldehydes. The synthesis of a shelf-stable (formylphenyl)bismuth reagent and its use in a cross-coupling reaction is also described.

European Journal of Organic Chemistry published new progress about Aryl halides Role: RCT (Reactant), RACT (Reactant or Reagent) (hetero-). 40353-41-1 belongs to class quinoxaline, name is 2-(Thiophen-2-yl)quinoxaline, and the molecular formula is C12H8N2S, Recommanded Product: 2-(Thiophen-2-yl)quinoxaline.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Xu, Yingying published the artcileIridium-Catalyzed Carbenoid Insertion of Sulfoxonium Ylides for Synthesis of Quinoxalines and β-Keto Thioethers in Water, Formula: C12H8N2S, the main research area is keto thioether green preparation carbenoid insertion annulation water; quinoxaline green preparation carbenoid insertion annulation water.

Sulfoxonium ylides as safe carbene precursors are described for iridium-catalyzed carbene insertions and annulation, providing a facile and green approach to access a variety of quinoxaline derivatives in water. This water-mediated method also allows the preparation of β-keto thioethers under mild condition.

European Journal of Organic Chemistry published new progress about Aromatic diamines Role: RCT (Reactant), RACT (Reactant or Reagent) (ortho). 40353-41-1 belongs to class quinoxaline, name is 2-(Thiophen-2-yl)quinoxaline, and the molecular formula is C12H8N2S, Formula: C12H8N2S.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Emmadi, Narender Reddy published the artcileSodium dodecylsulfate induced synthesis of quinoxalines, Related Products of quinoxaline, the main research area is quinoxaline preparation; phenylenediamine bromo ketone sodium dodecyl sulfate heterocyclization green chem.

A simple and efficient sodium dodecylsulfate (SDS) induced method for the synthesis of quinoxalines in excellent yields in water at room temperature by the reaction of phenacyl bromides and o-phenylene diamines was developed. Simple reaction conditions, wide compatibility and high yields were the advantages of this protocol.

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry published new progress about Alkyl aryl ketones Role: RCT (Reactant), RACT (Reactant or Reagent) (bromo). 40353-41-1 belongs to class quinoxaline, name is 2-(Thiophen-2-yl)quinoxaline, and the molecular formula is C12H8N2S, Related Products of quinoxaline.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Liu, Yun-Kui published the artcileRegiospecific Synthesis of Nitroarenes by Palladium-Catalyzed Nitrogen-Donor-Directed Aromatic C-H Nitration, Category: quinoxaline, the main research area is nitro arene regioselective preparation palladium catalyst; regioselective nitration arene nitrogen functional group guided.

Regioselective approach to nitroarenes involving palladium-catalyzed direct ortho-nitration of aromatic C-H bonds guided by a nitrogen functional group is described. E.g., Pd-catalyzed ortho-nitration of aromatic C-H bonds directed by a quinoxaline ligand (e.g., I) in presence of Pd(OAc)2, AgNO2, and K2S2O8 as oxidant gave 86% nitroarene II. The nitrating protocol was applied to other N-donor tethered aromatics [e.g., 2-arylpyridines, benzo[h]quinoline, 2-arylpyrazoles].

Chemistry – A European Journal published new progress about Aromatic nitro compounds Role: SPN (Synthetic Preparation), PREP (Preparation). 40353-41-1 belongs to class quinoxaline, name is 2-(Thiophen-2-yl)quinoxaline, and the molecular formula is C12H8N2S, Category: quinoxaline.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Ko, Kwangseok published the artcileDiscovery of a Novel Highly Selective Histamine H4 Receptor Antagonist for the Treatment of Atopic Dermatitis, Formula: C9H6Cl2N2, the main research area is atopic dermatitis H4 receptor antagonist preparation; pyrido tetrazolo pyrazine analog preparation atopic dermatitis.

The histamine H4 receptor (H4R), a member of the G-protein coupled receptor family, has been considered as a potential therapeutic target for treating atopic dermatitis (AD). A large number of H4R antagonists have been disclosed, but no efficient agents controlling both pruritus and inflammation in AD have been developed yet. Here, we have discovered a novel class of orally available H4R antagonists showing strong anti-itching and anti-inflammation activity as well as excellent selectivity against off-targets. A pharmacophore-based virtual screening system constructed in house successfully identified initial hit compound 9, and the subsequent homol. model-guided optimization efficiently led us to discover pyrido[2,3-e]tetrazolo[1,5-a]pyrazine analog 48 as a novel chemotype of a potent and highly selective H4R antagonist. Importantly, orally administered compound 48 exhibits remarkable efficacy on antipruritus and anti-inflammation with a favorable pharmacokinetic (PK) profile in several mouse models of AD. Thus, these data strongly suggest that our compound 48 is a promising clin. candidate for treatment of AD.

Journal of Medicinal Chemistry published new progress about 5-HT receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 39267-05-5 belongs to class quinoxaline, name is 2,3-Dichloro-6-methylquinoxaline, and the molecular formula is C9H6Cl2N2, Formula: C9H6Cl2N2.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Knudsen, Lotte Bjerre published the artcileSmall-molecule agonists for the glucagon-like peptide 1 receptor, SDS of cas: 25983-14-6, the main research area is glucagon like peptide receptor agonist thiadiazolyl quinoxaline preparation SAR.

The peptide hormone glucagon-like peptide (GLP)-1 has important actions resulting in glucose lowering along with weight loss in patients with type 2 diabetes. As a peptide hormone, GLP-1 has to be administered by injection. Only a few small-mol. agonists to peptide hormone receptors have been described and none in the B family of the G protein coupled receptors to which the GLP-1 receptor belongs. We have discovered a series of small mols. known as ago-allosteric modulators selective for the human GLP-1 receptor. These compounds act as both allosteric activators of the receptor and independent agonists. Potency of GLP-1 was not changed by the allosteric agonists, but affinity of GLP-1 for the receptor was increased. The most potent compound identified (I) stimulates glucose-dependent insulin release from normal mouse islets but, importantly, not from GLP-1 receptor knockout mice. Also, the compound stimulates insulin release from perfused rat pancreas in a manner additive with GLP-1 itself. These compounds may lead to the identification or design of orally active GLP-1 agonists.

Proceedings of the National Academy of Sciences of the United States of America published new progress about Glucagon receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 25983-14-6 belongs to class quinoxaline, name is 2,3,6,7-Tetrachloroquinoxaline, and the molecular formula is C8H2Cl4N2, SDS of cas: 25983-14-6.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Gan, Linling published the artcileTetrazanbigen Derivatives as Peroxisome Proliferator-Activated Receptor Gamma (PPARγ) Partial Agonists: Design, Synthesis, Structure-Activity Relationship, and Anticancer Activities, HPLC of Formula: 39267-05-5, the main research area is tetrazanbigen derivative peroxisome proliferator activated receptor gamma partial agonist; anticancer tetrazanbigen derivative.

Tetrazanbigen (TNBG) is a novel sterol isoquinoline derivative with poor water solubility and moderate inhibitory effects on human cancer cell lines via lipoapoptosis induction. Herein, we developed a series of novel TNBG analogs with improved water solubility and antiproliferative activities. The CCK-8 assay enabled us to identify a novel compound, 14g, which strongly inhibited HepG2 and A549 cell growth with IC50 values of 0.54 and 0.47μM, resp. The anticancer effects might be explained by the partial activation and upregulation of PPARγ expression, as indicated by the transactivation assay and western blotting evaluation. Furthermore, the in vitro antiproliferative activity was verified in an in vivo xenograft model in which 14g strongly reduced tumor growth at a dose of 10 mg/kg. In line with these pos. observations, 14g exhibited an excellent water solubility of 31.4 mg/mL, which was more than 1000-fold higher than that of TNBG (4μg/mL). Together, these results suggest that 14g is a promising anticancer therapeutic that deserves further investigation.

Journal of Medicinal Chemistry published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (PTEN). 39267-05-5 belongs to class quinoxaline, name is 2,3-Dichloro-6-methylquinoxaline, and the molecular formula is C9H6Cl2N2, HPLC of Formula: 39267-05-5.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Liu, Chun-He published the artcileDesign, synthesis, and biological evaluation of novel 4-alkylamino-1-hydroxymethylimidazo[1,2-a]quinoxalines as adenosine A1 receptor antagonists, HPLC of Formula: 25983-14-6, the main research area is oxoalkylamino chloroquinoxaline heterocyclization; imidazoquinoxaline preparation amine amination; aminoimidazoquinoxaline preparation adenosine receptor ligand.

A series of 4-alkylamino-1-hydroxymethylimidazo[1,2-a]quinoxalines, e.g., I, have been synthesized and evaluated for their adenosine A1 receptor inhibitory activity in the radioligand binding assays. These compounds were tested for the inhibition percent (IP) and the affinity toward A1AR (Ki) that IP were more than 90% in the nanomolar range. 4-Cyclopentylamino-7,8-dichloro-1-hydroxymethylimidazo[1,2-a]quinoxaline (I) was the most potent compound in this series, having Ki = 7 nM, which is remarkably higher than that of IRFI-165 (Ki = 48). 1-Hydroxymethyl groups of the tricyclic heteroaromatic compounds displayed the potent affinities toward A1AR.

Bioorganic & Medicinal Chemistry published new progress about Structure-activity relationship, purinergic receptor-binding. 25983-14-6 belongs to class quinoxaline, name is 2,3,6,7-Tetrachloroquinoxaline, and the molecular formula is C8H2Cl4N2, HPLC of Formula: 25983-14-6.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider