Month: November 2022

Pontillo, Joseph published the artcileSynthesis of aryl-1,2,4-triazine-3,5-diones as antagonists of the gonadotropin-releasing hormone receptor, Safety of 2-Methoxy-5-methylphenylboronic acid, the main research area is gonadotropin releasing hormone receptor antagonist aryl triazinedione preparation; aza uracil triazinedione preparation preparation gonadotropin releasing hormone receptor.

Several efficient synthetic routes for 2-, 4-, and 6-aryl-1,2,4-triazine-3,5-diones were developed. Derivatives were synthesized and studied as gonadotropin-releasing hormone antagonists in an effort to understand structure-activity relationships of the monocyclic compounds One compound was identified as potent gonadotropin-releasing hormone receptor antagonist from this series.

Bioorganic & Medicinal Chemistry Letters published new progress about Structure-activity relationship (gonadotropin-releasing hormone receptor antagonistic). 127972-00-3 belongs to class ethers-buliding-blocks, name is 2-Methoxy-5-methylphenylboronic acid, and the molecular formula is C8H11BO3, Safety of 2-Methoxy-5-methylphenylboronic acid.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Cerezo, Vanessa published the artcileSynthesis of 5-arylhistidines via a Suzuki-Miyaura cross-coupling, Synthetic Route of 127972-00-3, the main research area is histidine aryl regioselective synthesis microwave irradiation arylation bromination; bromohistidine Suzuki Miyaura cross coupling arylboronic acid palladium catalyst.

Microwave irradiation efficiently promoted the Suzuki-Miyaura reaction of a 5-bromohistidine with various arylboronic acids in the presence of a palladium catalyst. This methodol. allowed the synthesis of histidines substituted at position 5 of the imidazole ring with a Ph, a substituted Ph, a pyridyl or a thienyl ring. The corresponding 5-arylhistidines were obtained in moderate to good yields.

Tetrahedron published new progress about Aromatic compounds Role: RCT (Reactant), RACT (Reactant or Reagent). 127972-00-3 belongs to class ethers-buliding-blocks, name is 2-Methoxy-5-methylphenylboronic acid, and the molecular formula is C8H11BO3, Synthetic Route of 127972-00-3.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Okabe, Hiroyuki published the artcileAcceptor-Controlled Transfer Dehydration of Amides to Nitriles, Product Details of C3H7NO2, the main research area is palladium catalyzed transfer dehydration amide nitrile chloroacetonitrile water acceptor.

Palladium-catalyzed dehydration of primary amides to nitriles efficiently proceeds under mild, aqueous conditions via the use of dichloroacetonitrile as a water acceptor. A key to the design of this transfer dehydration catalysis is the identification of an efficient water acceptor, dichloroacetonitrile, that preferentially reacts with amides over other polar functional groups with the aid of the Pd catalyst and makes the desired scheme exergonic, thereby driving the dehydration.

Organic Letters published new progress about Chemoselectivity (of dehydration of amide group). 16332-06-2 belongs to class ethers-buliding-blocks, name is 2-Methoxyacetamide, and the molecular formula is C3H7NO2, Product Details of C3H7NO2.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Limberger, Jones published the artcileStereoselective synthesis of (E)-3,3-diaryl and (E)-3-aryl-3-aryloxy allylamines and allylalcohols from trans-cinnamyl chloride and alcohol, Formula: C8H11BO3, the main research area is diaryl allylamine regioselective diastereoselective preparation Suzuki coupling; aryl aryloxy allylamine regioselective diastereoselective preparation Ullmann coupling; allylalc diaryl regioselective diastereoselective preparation Suzuki coupling; aryloxy aryl allylalc regioselective diastereoselective preparation Ullmann coupling.

The regio and stereoselective synthesis of (E)-3,3-diaryl and (E)-3-aryl-3-aryloxy allylamines and allylalcs was described. The starting materials were the non-expensive com. available cinnamyl alc. and chloride. The bromination/dehydrobromination sequence furnished the (E)-3-bromo-3-phenylallyl amines and alc. as single regioisomers and with high stereoselectivity (>98%). These vinyl bromides were used as substrates in cross-coupling reactions furnishing the arylated products with good to excellent yields and total E-configuration retention. Regio and stereospecifically trisubstituted olefins and vinyl ethers by Suzuki cross-coupling and Ullmann vinylation were produced.

RSC Advances published new progress about Allylic alcohols Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 127972-00-3 belongs to class ethers-buliding-blocks, name is 2-Methoxy-5-methylphenylboronic acid, and the molecular formula is C8H11BO3, Formula: C8H11BO3.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Hodgetts, Kevin J. published the artcileDiscovery of N-(1-Ethylpropyl)-[3-methoxy-5-(2-methoxy-4-trifluoromethoxyphenyl)-6-methyl-pyrazin-2-yl]amine 59 (NGD 98-2): An Orally Active Corticotropin Releasing Factor-1 (CRF-1) Receptor Antagonist, Application In Synthesis of 127972-00-3, the main research area is pyrazine preparation SAR CRF 1 receptor antagonist; orally active corticotropin releasing factor 1 receptor antagonist.

The design, synthesis, and structure-activity relationships of a novel series of pyrazines, acting as corticotropin releasing factor-1 (CRF-1) receptor antagonists, are described. Synthetic methodologies were developed to prepare a number of substituted pyrazine cores utilizing regioselective halogenation and chemoselective derivatization. Noteworthy, an efficient 5-step synthesis was developed for the lead compound I (NGD 98-2), which required no chromatog. Compound I was characterized as an orally bioavailable, brain penetrant, and highly selective CRF-1 receptor antagonist. Occupancy of rat brain CRF-1 receptors was quantified using ex vivo receptor occupancy assays, using both brain tissue homogenates as well as brain slices receptor autoradiog. Behaviorally, oral administration of I significantly antagonized CRF-induced locomotor activity at doses as low as 10 mg/kg and dose-dependently reduced the restraint stress-induced ACTH increases.

Journal of Medicinal Chemistry published new progress about Homo sapiens. 127972-00-3 belongs to class ethers-buliding-blocks, name is 2-Methoxy-5-methylphenylboronic acid, and the molecular formula is C8H11BO3, Application In Synthesis of 127972-00-3.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Yue, Yuanyuan published the artcileElectrooxidative double C-H/C-H coupling of phenols with 3-phenylbenzothiophenes: facile access to benzothiophene derivatives, Computed Properties of 121-00-6, the main research area is benzothiophene preparation; phenol phenylbenzothiophene electrooxidative oxidant catalyst free.

An efficient electrooxidative double C-H/C-H coupling of phenols with 3-phenylbenzothiophene has been developed under external oxidant- and catalyst-free conditions. This strategy could enable the highly tunable access to benzothiophene derivatives and exhibited broad substrate generality under mild conditions. The reaction is likely to proceed via the cross-coupling of the p-methoxylphenol radical and the 3-phenylbenzothiophene radical cation.

Organic & Biomolecular Chemistry published new progress about Electrooxidative coupling reaction. 121-00-6 belongs to class ethers-buliding-blocks, name is 4-Hydroxy-3-tert-butylanisole, and the molecular formula is C11H16O2, Computed Properties of 121-00-6.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Purtsas, Alexander published the artcileIron-Catalyzed Oxidative C-O and C-N Coupling Reactions Using Air as Sole Oxidant, Application In Synthesis of 121-00-6, the main research area is tertiary arylamine phenol hexadecafluorophthalocyanine iron catalyst regioselctive oxidative coupling; diaryl ether preparation; phenothiazine tertiary arylamine hexadecafluorophthalocyanine iron catalyst regioselctive oxidative coupling; phenothiazinyl aryl amine preparation; phenolphenothiazine hexadecafluorophthalocyanine iron catalyst regioselctive oxidative coupling; phenothiazinylphenol preparation; C−H activation; air; homogeneous catalysis; iron; oxidative amination.

The oxygenation of tertiary arylamines, and the amination of tertiary arylamines and phenols was described. The key step of these coupling reactions was an iron-catalyzed oxidative C-O or C-N bond formation which generally provides the corresponding products in high yields and with excellent regioselectivity. The transformations were accomplished using hexadecafluorophthalocyanine-iron(II) (FePcF16) as catalyst in the presence of an acid or a base additive and require only ambient air as sole oxidant.

Chemistry – A European Journal published new progress about Aromatic ethers Role: PRP (Properties), SPN (Synthetic Preparation), PREP (Preparation). 121-00-6 belongs to class ethers-buliding-blocks, name is 4-Hydroxy-3-tert-butylanisole, and the molecular formula is C11H16O2, Application In Synthesis of 121-00-6.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Carreras, Lucas published the artcileSelective functionalisation of aromatic alcohols with supramolecularly regulated gold(I) catalysts, Recommanded Product: 2,5,8,11-Tetraoxatridecan-13-ol, the main research area is hydroxyaryl carbonyl derivative preparation gold catalyst; aromatic alc diazo ester carbon hydrogen insertion reaction.

Phosphite-based Au(I) catalytic systems containing an array of structurally diverse polyether-based regulation sites were designed and synthesized. These catalysts have been successfully tested in the Au(I)-catalyzed C-H functionalization of phenols and related derivatives with gold-carbenes derived from diazo compounds Regulation of the steric congestion around the catalytic Au(I) center via ion-dipole interactions with an external regulation agent led to an enhancement of both the activity and selectivity of the reaction. This new approach in supramol. gold(I) catalysis has been applied to the derivatisation of an array of substituted phenols and related substrates and to the preparation of an advanced synthetic intermediate of the anticancer agent tamoxifen. The effects of the regulation agent on the selectivity and yield of the reaction have been studied and rationalised using DFT-D calculations

Organic Chemistry Frontiers published new progress about Aromatic alcohols Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 23783-42-8 belongs to class ethers-buliding-blocks, name is 2,5,8,11-Tetraoxatridecan-13-ol, and the molecular formula is C9H20O5, Recommanded Product: 2,5,8,11-Tetraoxatridecan-13-ol.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Davies, Christopher J. published the artcileUse of Suzuki cross-coupling as a route to 2-phenoxy-6-iminopyridines and chiral 2-phenoxy-6-(methanamino)pyridines, Related Products of ethers-buliding-blocks, the main research area is anisyl boronic acid carbonyl bromopyridine Suzuki coupling; phenoxycarbonylpyridine derivative preparation diisopropylaniline imination; phenoxyiminopyridine derivative preparation crystal structure methyllithium nucleophilic addition reduction; pyridine phenoxyimino derivative preparation trimethylaluminum nucleophilic addition reduction; methanaminopyridine phenoxy derivative preparation crystal structure.

The anisyl boronic acids I (R1 = R2 = H; R1 = H, R2 = Ph; R1 = Me, R2 = H; R1 = Cl, R2 = H; R1 = t-Bu, R2 = H), have been employed in Suzuki cross-coupling reactions with either 2-bromo-6-formylpyridine or 2-bromo-6-acetylpyridine generating, following a facile deprotection step, the 2-phenoxy-6-carbonylpyridines II (R1 = R2 = H; R1 = Me, R2 = H; R1 = Cl, R2 = H; R1 = t-Bu, R2 = H) and III (R1 = R2 = H; R1 = H, R2 = Ph). Condensation reactions of II and III with 2,6-diisopropylaniline proceed smoothly to give the corresponding 2-phenoxy-6-iminopyridines. Reduction of the imino unit of the imines derived from II (and concomitant C-C bond formation) can be achieved by treatment with trimethylaluminum or methyllithium which, following hydrolysis, furnishes the racemic chiral 2-phenoxy-6-(methanamino)pyridines IV (R1 = R2 = H; R1 = Me, R2 = H; R1 = Cl, R2 = H; R1 = t-Bu, R2 = H). This work represents a straightforward and rapid synthetic route to libraries of sterically and electronically variable phenoxy-substituted imino- and methanamino-pyridines, which are expected to act as useful ligands or proligands for late and early transition metal-mediated alkene polymerization catalysis.

Tetrahedron published new progress about Aromatic amines Role: SPN (Synthetic Preparation), PREP (Preparation) (pyridinylmethyl). 127972-00-3 belongs to class ethers-buliding-blocks, name is 2-Methoxy-5-methylphenylboronic acid, and the molecular formula is C8H11BO3, Related Products of ethers-buliding-blocks.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Dovlatyan, V. V. published the artcileSome conversions of thiazoline carboxylic acid esters, HPLC of Formula: 622-86-6, the main research area is methylthioxothiazoline hydrazone synthesis; thiazoline carboxylate solvolysis hydrazinolysis.

The authors have carried out solvolysis of the previously described Et esters of 3-methyl(aryl)-4-methyl-2-thioxothiazoline-5-carboxylic acids, leading to the corresponding acids without breaking down the heterocycle. They synthesized a series of novel esters from the latter by treatment with di-Me sulfate or reactive halides. Of these, only in the case of the Et ester of 3,4-dimethyl-2-thioxothiazoline-5-carboxylic acid did they obtain the hydrazinolysis product (the hydrazide), from which they synthesized novel hydrazones by treatment with aldehydes and ketones.

Chemistry of Heterocyclic Compounds published new progress about Hydrazinolysis. 622-86-6 belongs to class ethers-buliding-blocks, name is (2-Chloroethoxy)benzene, and the molecular formula is C8H9ClO, HPLC of Formula: 622-86-6.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem