Category: 143426-50-0

Artico, M. published the artcileAromatic hydrazides as specific inhibitors of bovine serum amine oxidase, Quality Control of 143426-50-0, the main research area is aromatic hydrazide preparation amine oxidase inhibitor; structure activity hydrazide oxidase inhibitor.

New hydrazides were synthesized in search for specific inhibitors of bovine serum amine oxidase: a series of benzoic and phenylacetic acid hydrazides containing the 1H-imidazol-1-yl or the 1H-imidazol-1-ylmethyl group as as o-, m-, or p-substituent in the Ph ring; an analogous series of p-substituted phenylhydrazides with a 5 or 6-membered heterocyclic ring substituent, and a series of similar phenylpropionic hydrazides. The longer and more flexible phenylacetic hydrazides, and to a somewhat lesser extent the phenylpropionic ones, were better specific inhibitors of bovine serum amine oxidase than the benzoic hydrazides, which were also bound by the enzyme with high affinity, but at a slow rate. Derivatives with p- and m-substituents were more reactive than the o-substituted ones. The chem. nature of the substituent was less important than its position in the Ph ring and the presence of methylene spacers. These data point to the presence of a hydrophobic site at short distance from the protein carbonyl cofactor, so that simultaneous interaction of the 2 ends of the inhibitor mol. can occur at the 2 sites. The presence of the hydrophobic site was confirmed by the capability of some mols. deprived of the hydrazidic group to act as mild inhibitors. All hydrazides were less reactive by 2-3 orders of magnitude towards pig kidney diamine oxidase and FAD-dependent monoamine oxidase from rat brain mitochondria, while the other compounds showed similar inhibition power against all proteins. The specificity for the bovine enzyme seems therefore to be related to the concerted action of the 2 moieties of the inhibitor mol.

European Journal of Medicinal Chemistry published new progress about aromatic hydrazide preparation amine oxidase inhibitor; structure activity hydrazide oxidase inhibitor. 143426-50-0 belongs to class triazoles, name is 4-(1,2,4-Triazol-1-yl)benzyl Alcohol, and the molecular formula is C9H9N3O, Quality Control of 143426-50-0.

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Sekioka, Ryuichi published the artcileDiscovery of N-ethylpyridine-2-carboxamide derivatives as a novel scaffold for orally active γ-secretase modulators, Name: 4-(1,2,4-Triazol-1-yl)benzyl Alcohol, the main research area is Alzheimer’s disease gamma secretase modulator myloid beta peptide; Alzheimer’s disease; Amyloid-beta peptide; Cytochrome P450 3A4; Gamma-secretase modulator.

Gamma-secretase modulators (GSMs) are promising disease-modifying drugs for Alzheimer’s disease because they can selectively decrease pathogenic amyloid-β42 (Aβ42) levels. Here we report the discovery of orally active N-ethylpyridine-2-carboxamide derivatives as GSMs. The isoindolinone moiety of 5-[8-(benzyloxy)-2-methylimidazo[1,2-a]pyridin-3-yl]-2-ethyl-2,3-dihydro-1H-isoindol-1-one hydrogen chloride (1a) was replaced with a picolinamide moiety. Optimization of the benzyl group significantly improved GSM activity and mouse microsomal stability. 5-{8-[([1,1′-Biphenyl]-4-yl)methoxy]-2-methylimidazo[1,2-a]pyridin-3-yl}-N-ethylpyridine-2-carboxamide hydrogen chloride (1v) potently reduced Aβ42 levels with an IC50 value of 0.091μM in cultured cells without inhibiting CYP3A4. Moreover, 1v demonstrated a sustained pharmacokinetic profile and significantly reduced brain Aβ42 levels in mice.

Bioorganic & Medicinal Chemistry published new progress about Alzheimer disease. 143426-50-0 belongs to class triazoles, name is 4-(1,2,4-Triazol-1-yl)benzyl Alcohol, and the molecular formula is C9H9N3O, Name: 4-(1,2,4-Triazol-1-yl)benzyl Alcohol.

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Iwamura, Ryo published the artcileIdentification of a Selective, Non-Prostanoid EP2 Receptor Agonist for the Treatment of Glaucoma: Omidenepag and its Prodrug Omidenepag Isopropyl, SDS of cas: 143426-50-0, the main research area is prostanoid EP2 receptor agonist preparation glaucoma.

EP2 receptor agonists are expected to be effective ocular hypotensive agents; however, it has been suggested that agonism to other EP receptor subtypes may lead to undesirable effects. Through medicinal chem. efforts, we identified a scaffold bearing a (pyridin-2-ylamino)acetic acid moiety as a promising EP2-selective receptor agonist. (6-((4-(Pyrazol-1-yl)benzyl)(pyridin-3-ylsulfonyl)aminomethyl)pyridin-2-ylamino)acetic acid 13ax (omidenepag, OMD) exerted potent and selective activity toward the human EP2 receptor (h-EP2). Low doses of omidenepag iso-Pr (OMDI), a prodrug of 13ax, lowered intraocular pressure (IOP) in ocular normotensive monkeys. OMDI was selected as a clin. candidate for the treatment of glaucoma.

Journal of Medicinal Chemistry published new progress about Antiglaucoma agents. 143426-50-0 belongs to class triazoles, name is 4-(1,2,4-Triazol-1-yl)benzyl Alcohol, and the molecular formula is C9H9N3O, SDS of cas: 143426-50-0.

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Liu, Luxiao published the artcileDeep eutectic solvent promoted one-pot synthesis of nitriles from alcohols, Category: triazoles, the main research area is aryl nitrile green preparation; alc tandem aerobic oxidation condensation deep eutectic solvent.

Various aryl nitriles RCN [R = Ph, 4-BrC6H4, 2-thienyl, etc.] were readily synthesized from aerobic oxidation of substituted benzyl alcs. in deep eutectic solvent composed of choline chloride and p-toluenesulfonic acid in the presence of 2,2,6,6-tetramethylpiperidine-1-oxyl, followed by condensation with hydroxylamine hydrochloride. High yields of corresponding nitriles had obtained under mild reactions conditions. This strategy belonged to a novel and environmentally benign transition-metal-free one-pot cascade process for the synthesis of nitriles.

Journal of Chemical Sciences (Berlin, Germany) published new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 143426-50-0 belongs to class triazoles, name is 4-(1,2,4-Triazol-1-yl)benzyl Alcohol, and the molecular formula is C9H9N3O, Category: triazoles.

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Nugent, Jeremy published the artcileA General Route to Bicyclo[1.1.1]pentanes through Photoredox Catalysis, Application In Synthesis of 143426-50-0, the main research area is bicyclopentane preparation photoredox catalyst halide carbocyclepropellane addition.

Photoredox catalysis has transformed the landscape of radical-based synthetic chem. Additions of radicals generated through photoredox catalysis to carbon-carbon π-bonds are well-established; however, this approach has yet to be applied to the functionalization of carbon-carbon σ-bonds. Here, the authors report the first such use of photoredox catalysis to promote the addition of organic halides to the carbocycle [1.1.1]propellane; the product bicyclo[1.1.1]pentanes (BCPs) are motifs of high importance in the pharmaceutical industry and in materials chem. Showing broad substrate scope and functional group tolerance, this methodol. results in the first examples of bicyclopentylation of sp2 carbon-halogen bonds to access (hetero)arylated BCPs, as well as the functionalization of nonstabilized sp3 radicals. Substrates containing alkene acceptors allow the single-step construction of polycyclic bicyclopentane products through unprecedented atom transfer radical cyclization cascades, while the potential to accelerate drug discovery is demonstrated through late-stage bicyclopentylations of natural product-like and drug-like mols. Mechanistic studies demonstrate the importance of the photocatalyst in this chem. and provide insight into the balance of radical stability and strain relief in the reaction cycle.

ACS Catalysis published new progress about Photocatalysts. 143426-50-0 belongs to class triazoles, name is 4-(1,2,4-Triazol-1-yl)benzyl Alcohol, and the molecular formula is C9H9N3O, Application In Synthesis of 143426-50-0.

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Hu, Yongke published the artcileDirect oxidative esterification of alcohols catalyzed by a nitrogen-doped carbon black-supported PdBi bimetallic catalyst under ambient conditions, SDS of cas: 143426-50-0, the main research area is PdBi bimetallic catalyzed oxidative esterification alc; aryl ester preparation PdBi bimetallic catalyzed oxidative esterification.

A highly efficient nitrogen-doped carbon black (NCB)-supported PdBi alloy nanocatalyst has been fabricated via a facile coredn. wet chem. approach. The optimal PdBi/NCB shows outstanding catalytic performance with broad substrate scope, good functional group tolerance towards direct oxidative esterification of alcs. under mild conditions in a heterogeneous catalytic system with air as the sole oxidant. A variety of benzylic and allylic alcs. were smoothly reacted with methanol and even with long-chain aliphatic alcs., providing desired esters in good to excellent yields. Moreover, the as-prepared catalyst is easily recycled and can be reused at least five times without a significant loss of catalytic activity. Superior catalytic activity is mainly attributable to the unique structure of the catalyst, including synergetic electronic effect between Pd and Bi, as well as modulated surface character by acidification and N doping for better active components’ anchoring and dispersion, as well as reactants’ adsorption. This study provides a facial, practical, eco-friendly and efficient catalytic system for oxidative esterification of alcs. and shows promising prospect in industrial production

Journal of Materials Science published new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 143426-50-0 belongs to class triazoles, name is 4-(1,2,4-Triazol-1-yl)benzyl Alcohol, and the molecular formula is C9H9N3O, SDS of cas: 143426-50-0.

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Lou, Ji-Cong published the artcileMetal-Free Oxidation of Trichloroacetimidates to Aldehydes, HPLC of Formula: 143426-50-0, the main research area is alc trichloroacetonitrile DBU imidation; trichloroacetimidate preparation dimethylsulfoxide oxidation; carbonyl compound preparation.

A metal-free oxidation reaction of trichloroacetimidates to aldehydes or ketones with DMSO as an oxidant was reported. The reaction exhibited a broad range of functional group tolerance. Detailed mechanistic studies were performed with the aid of NMR, in-situ IR spectroscopy, GC-MS anal. and 18O-labeling experiments

Asian Journal of Organic Chemistry published new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 143426-50-0 belongs to class triazoles, name is 4-(1,2,4-Triazol-1-yl)benzyl Alcohol, and the molecular formula is C9H9N3O, HPLC of Formula: 143426-50-0.

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Hu, Yongke published the artcilePractical CuCl/DABCO/4-HO-TEMPO-catalyzed oxidative synthesis of nitriles from alcohols with air as oxidant, Application In Synthesis of 143426-50-0, the main research area is copper chloride DABCO TEMPO oxidation alc; nitrile preparation green.

A mild and efficient methodol. for the direct oxidative synthesis of nitriles from easily available alcs. and aqueous ammonia by employing CuCl/DABCO/4-HO-TEMPO as the catalysts is described. This protocol uses the air as a green oxidant and aqueous ammonia as the nitrogen source at room temperature A variety of aryl, heterocyclic and allylic alcs. are smoothly converted into the corresponding nitriles in good to excellent yields.

Chinese Chemical Letters published new progress about Aralkyl alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 143426-50-0 belongs to class triazoles, name is 4-(1,2,4-Triazol-1-yl)benzyl Alcohol, and the molecular formula is C9H9N3O, Application In Synthesis of 143426-50-0.

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Hu, Yongke published the artcileEfficient and selective palladium-catalyzed direct oxidative esterification of benzylic alcohols under aerobic conditions, COA of Formula: C9H9N3O, the main research area is aliphatic benzylic alc oxidative esterification palladium; alkyl benzoate preparation; palladium oxidative esterification catalyst.

A highly efficient palladium-catalyzed approach for the direct oxidative esterification of benzylic alcs. with methanol and long-chain aliphatic alcs. under mild conditions has been achieved. This practical catalyst system exhibits a broad substrate scope and good functional group tolerance. Catalytic amount of Bi(OTf)3 is used as co-catalyst to improve the activity and selectivity of the reactions. A variety of esters are obtained in yields of 43-96%.

Tetrahedron published new progress about Aliphatic alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 143426-50-0 belongs to class triazoles, name is 4-(1,2,4-Triazol-1-yl)benzyl Alcohol, and the molecular formula is C9H9N3O, COA of Formula: C9H9N3O.

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Yin, Weiyu published the artcileHighly Practical Synthesis of Nitriles and Heterocycles from Alcohols under Mild Conditions by Aerobic Double Dehydrogenative Catalysis, HPLC of Formula: 143426-50-0, the main research area is alc aerobic double dehydrogenation ammonia nitrile synthesis; biaryl heterocycle one pot synthesis nitrile in situ heterocyclization.

A mild, aerobic, catalytic process for obtaining nitriles directly from alcs. and aqueous ammonia is described (RC6H4CH2OH + NH3 → RC6H4CN). The reaction proceeds via a dehydrogenation cascade mediated by catalytic CuI, bpy, and TEMPO in the presence of O2. The substrate scope is broad including various functionalized aromatic and aliphatic alcs. This protocol enabled the one-pot synthesis of various biaryl heterocycles directly from com. available alcs. (e.g., PhCH2OH + NH3 in first step; addition of ethylenediamine in second step → 2-phenyl-4,5-dihydro-1H-imidazole).

Organic Letters published new progress about Aliphatic alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 143426-50-0 belongs to class triazoles, name is 4-(1,2,4-Triazol-1-yl)benzyl Alcohol, and the molecular formula is C9H9N3O, HPLC of Formula: 143426-50-0.

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics