Category: 127972-00-3

Wu, Zhao published the artcileAsymmetric synthesis of γ-branched amines via rhodium-catalyzed reductive amination, Safety of 2-Methoxy-5-methylphenylboronic acid, the main research area is amine rhodium catalyst tandem chemoselective enantioselective reductive amination.

A general asym. route for the one-pot synthesis of chiral γ-branched amines through the highly enantioselective isomerization of allylamines, followed by enamine exchange and subsequent chemoselective reduction was reported. This protocol was suitable for establishing various tertiary stereocenters, including those containing dialkyl, diaryl, cyclic, trifluoromethyl, difluoromethyl, and silyl substituents, which allowed for a rapid and modular synthesis of many chiral γ-branched amines. To demonstrate the synthetic utility, Terikalant and Tolterodine were synthesized using this method with high levels of enantioselectivity.

Nature Communications published new progress about Amines, unsaturated 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, Safety of 2-Methoxy-5-methylphenylboronic acid.

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

Khalaf, Juhienah published the artcileDesign, Synthesis, and Diversification of 3,5-Substituted Enone Library, Quality Control of 127972-00-3, the main research area is enone combinatorial library preparation; bromoenone preparation boronic acid Suzuki coupling; terminal alkyne bromoenone Sonogashira coupling; triazole preparation.

This paper describes the synthesis of a 300 member library of 3,5-substituted enones, e.g., I. The synthesis starts with six different bromoenones that are accessed from the corresponding 1,3 diones. These bromides are then diversified by Suzuki coupling with a variety of aromatic and vinyl boronic acids. Addnl. a small series of triazoles, e.g., II, were synthesized by a Sonogashira coupling reaction dipolar cycloaddition sequence. The library was analyzed by principal component anal. to examine its diversity.

ACS Combinatorial Science published new progress about Alkynes, α- 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, Quality Control of 127972-00-3.

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

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

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

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

Eastman, Brian published the artcileExpedited SAR study of an mGluR5 antagonists: generation of a focused library using a solution-phase Suzuki coupling methodology, SDS of cas: 127972-00-3, the main research area is phenyltetrazolyl pyridine preparation mGluR5 antagonist structure.

The SAR of the lead compounds I (R = H) and I (R = F) was rapidly explored. Utilizing a parallel solution-phase Suzuki coupling approach, in tandem with strong cation exchange resin (SCX) purification afforded the desired focused library. The library was evaluated in vitro, a ninefold potency increase was achieved and the preference for ortho substitution of moderate steric bulk of the fourth, Ph ring was identified. In addition, dimethylisoxazole, as a heterocyclic replacement for the phenylic ring of the lead compound, was also identified by this approach.

Bioorganic & Medicinal Chemistry Letters published new progress about Structure-activity relationship. 127972-00-3 belongs to class ethers-buliding-blocks, name is 2-Methoxy-5-methylphenylboronic acid, and the molecular formula is C8H11BO3, SDS of cas: 127972-00-3.

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

Yuan, Shuqing published the artcileChromium-Catalyzed Reductive Cleavage of Unactivated Aromatic and Benzylic C-O Bonds, Application In Synthesis of 127972-00-3, the main research area is pyridinylphenyl ether chromium catalyst reductive deoxygenation; methoxymethylnaphthalene chromium catalyst reductive deoxygenation.

Reductive cleavage of aromatic and benzylic C-O bonds by chromium catalysis was reported. This deoxygenative reaction was promoted by low-cost CrCl2 precatalyst combined with poly(Me hydrogen siloxane) as the mild reducing agent, providing a strategy in forming reduced motifs by cleavage of unactivated C-O bonds. A range of functional groups such as bromide, chloride, fluoride, hydroxyl, amino and alkoxycarbonyl was retained in the reduction

Synthesis published new progress about Arylboronic acids 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, Application In Synthesis of 127972-00-3.

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