Category: 52244-70-9

Lu, Jiayu; Wang, Xiangjun; Ge, Shuai; Hou, Yajing; Lv, Yuexin; He, Huaizhen; Wang, Cheng published the artcile< Synthesis and evaluation of new potential anti-pseudo-allergic agents>, Recommanded Product: 4-(4-Methoxyphenyl)-1-butanol, the main research area is anti pseudo allergy mubritinib MRGPRX2 receptor; B10-S; MRGPRX2; Mast cells; Mubritinib; Pseudo-allergy.

Pseudo-allergic reactions frequently occur following clin. drug use and sometimes even cause mortal danger. Mas-related G-protein-coupled receptor member X2 (MRGPRX2) is a novel receptor that mediates pseudo-allergy and is an important target in the treatment of allergies. However, to date, there are no synthetic small-mol. inhibitors that prevent anaphylactoid reactions through this pathway. Our preliminary research suggested that B10-S and mubritinib effectively inhibited LAD2 cells. Therefore, two novel derivatives were synthesized by integrating the active substructures of B10-S and mubritinib, according to the mol. docking results. The antiallergic inhibitory effects of the two compounds were preliminarily evaluated in vitro using β-hexosaminidase release, histamine release, and intracellular Ca2+ mobilization assays, and their binding sites on MRGPRX2 were analyzed by mol. docking. Both substances inhibited β-hexosaminidase and histamine release in LAD2 cells and decreased intracellular Ca2+ by inhibiting MRGPRX2 in MRGPRX2-HEK293 cells treated with C48/80 in a dose-dependent manner. The docking results suggested that the mols. could competitively bind to the active site on MRGPRX2 and Glu141, which were combined by C48/80. Our study indicated that the two compounds have potential anti-allergic properties, which may provide evidence that will facilitate the development of synthetic mols. with anti-pseudo-allergic activity for clin. use in the future.

Bioorganic & Medicinal Chemistry Letters published new progress about Allergy. 52244-70-9 belongs to class ethers-buliding-blocks, and the molecular formula is C11H16O2, Recommanded Product: 4-(4-Methoxyphenyl)-1-butanol.

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

Kim, Byung Hyun; Lee, Jong Gil; Kim, Woon Ki; Kim, Young Gyu published the artcile< Regioselective Synthesis of 2,6-Dimethyltetralin: Key Precursor to 2,6-Dimethylnaphthalene>, Quality Control of 52244-70-9, the main research area is tetralin dimethyl regioselective preparation; naphthalene dimethyl regioselective preparation; tetrahydronaphthalene regioselective preparation; alc arylbutyl preparation intramol Friedel Crafts alkylation.

A novel regioselective synthesis for 2,6-dimethyltetralin (2,6-DMT), a key precursor to 2,6-dimethylnaphthalene (2,6-DMN), is described. The synthesis comprises the following three steps; the Heck reaction between com. available 4-bromotoluene and 3-methyl-3-buten-1-ol, the catalytic reduction of the coupling products, and the acid-catalyzed cyclization of the alc. intermediate. The process has an advantage over the established processes in that 2,6-DMT is obtained as the only isomer, and the isomerization and/or the complicated separation and purification steps are not required to produce pure 2,6-DMT. 2,6-DMN could be also obtained as a major product depending on the cyclization conditions.

Organic Process Research & Development published new progress about Aralkyl alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 52244-70-9 belongs to class ethers-buliding-blocks, and the molecular formula is C11H16O2, Quality Control of 52244-70-9.

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

Kende, Andrew S.; Koch, Kevin published the artcile< Intramolecular radical cyclization of phenolic nitronates. Facile synthesis of annelated tropone and tropolone derivatives>, Electric Literature of 52244-70-9, the main research area is nitrophenolate electron transfer cyclization; spirocyclic nitro dienone preparation rearrangement; bicyclic tropone.

Treating p-HOC6H4(CH2)nNO2 (n = 4, 5) or 4,3-HO(MeO)C6H3(CH2)4NO2 with aqueous KOH followed by K3Fe(CN)6 gives spirocyclic nitrodienones I (X = CH2, CH2CH2; R = H, OMe), which rearrange to bicyclic tropones II (same X, R).

Tetrahedron Letters published new progress about Cycloaddition reaction, intramolecular. 52244-70-9 belongs to class ethers-buliding-blocks, and the molecular formula is C11H16O2, Electric Literature of 52244-70-9.

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

Ondrejkova, Alica; Lindroth, Rickard; Hilmersson, Goeran; Wallentin, Carl-Johan published the artcile< Utilizing a needle as a source of iron in synergistic dual photoredox catalytic generation of alkoxy radicals>, Related Products of 52244-70-9, the main research area is THF bromoketone preparation photoredox iron synergistic catalysis.

A visible-light mediated alkoxy radical generation is described, which allows for a structurally divergent oxidative C(sp3)-H bond functionalization. This protocol employs a photoredox/iron dual catalysis allowing for an unprecedented chemoselective single-step transformation of alc. derivatives giving access to two valuable sets of products, tetrahydrofurans and γ-bromoketones, under one set of conditions. Addition of iron, by slow corrosion of a needle, provides superior reaction efficiency as compared to various iron(III) complexes.

Chemical Communications (Cambridge, United Kingdom) published new progress about C-H bond activation. 52244-70-9 belongs to class ethers-buliding-blocks, and the molecular formula is C11H16O2, Related Products of 52244-70-9.

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

Kosui, Nobuo; Waki, Michinori; Kato, Tetsuo; Izumiya, Nobuo published the artcile< Preparation of homologs of L-2-amino-5-(p-methoxyphenyl)pentanoic acid>, Quality Control of 52244-70-9, the main research area is aminoalkanoic acid anisyl; anisylalkanoic acid amino; butanoic acid aminoanisyl; hexanoic acid aminoanisyl; resolution acetamidoanisylalkanoic acid deacetylation; enzyme resolution acetamidoanisylalkanoic acid.

L-p-MeOC6H4(CH2)nCH(NH2)CO2H (n = 2, 4) were prepared by optical resolution of their N-acetyl derivatives with Aspergillus acylase. The N-acetyl derivatives were synthesized from p-MeO6H4(CH2)nC(NHAc)(CO2H)2 by heating with p-xylene.

Bulletin of the Chemical Society of Japan published new progress about 52244-70-9. 52244-70-9 belongs to class ethers-buliding-blocks, and the molecular formula is C11H16O2, Quality Control of 52244-70-9.

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

Zheng, Guangrong; Smith, Andrew M.; Huang, Xiaoqin; Subramanian, Karunai L.; Siripurapu, Kiran B.; Deaciuc, Agripina; Zhan, Chang-Guo; Dwoskin, Linda P. published the artcile< Structural Modifications to Tetrahydropyridine-3-carboxylate Esters en Route to the Discovery of M5-Preferring Muscarinic Receptor Orthosteric Antagonists>, Recommanded Product: 4-(4-Methoxyphenyl)-1-butanol, the main research area is tetrahydropyridine carboxylate ester preparation muscarinic receptor drug abuse.

The M5 muscarinic acetylcholine receptor is suggested to be a potential pharmacotherapeutic target for the treatment of drug abuse. We describe herein the discovery of a series of M5-preferring orthosteric antagonists based on the scaffold of 1,2,5,6-tetrahydropyridine-3-carboxylic acid. Compound 56, the most selective compound in this series, possesses an 11-fold selectivity for the M5 over M1 receptor and shows little activity at M2-M4. This compound, although exhibiting modest affinity (Ki = 2.24 μM) for the [3H]N-methylscopolamine binding site on the M5 receptor, is potent (IC50 = 0.45 nM) in inhibiting oxotremorine-evoked [3H]DA release from rat striatal slices. Further, a homol. model of human M5 receptor based on the crystal structure of the rat M3 receptor was constructed, and docking studies of compounds 28 and 56 were performed in an attempt to understand the possible binding mode of these novel analogs to the receptor.

Journal of Medicinal Chemistry published new progress about Drugs of abuse. 52244-70-9 belongs to class ethers-buliding-blocks, and the molecular formula is C11H16O2, Recommanded Product: 4-(4-Methoxyphenyl)-1-butanol.

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

Liu, Jie; Xiang, Haonan; Jiang, Lvqi; Yi, Wenbin published the artcile< Chemoselective desulfurization-fluorination/bromination of carbonofluoridothioates for the O-trifluoromethylation and O-bromodifluoromethylation of alcohols>, Electric Literature of 52244-70-9, the main research area is carbonofluoridothioate preparation desulfurization fluorination bromination; bromodifluoromethyl ether alkyl preparation chemoselective; alkyl trifluoromethyl ether preparation chemoselective; alc trifluoromethylation.

Herein, a method for synthesizing various alkyl trifluoromethyl e.g., C6H5(CH2)5OCF3 and alkyl bromodifluoromethyl ethers e.g., C6H5(CH2)5OCF2Br using carbonofluoridothioates e.g., C6H5(CH2)5OC(S)F as precursors has been described. Carbonofluoridothioates were obtained upon the reaction of an alc. e.g., C6H5(CH2)5OH and S=CF2 generated via the decomposition of an SCF3 anion, and then selectively transformed into their corresponding trifluoromethyl and bromodifluoromethyl ethers upon changing the reaction conditions. This transformation has also been extended to the one-pot, two-step conversion of alcs. into alkyl trifluoromethyl ethers. A series of alkyl bromodifluoromethyl ethers has also been synthesized. These compounds open up a new avenue for the synthesis of a wide range of useful fluorinated products. In addition, this method is suitable for the late-stage introduction of trifluoromethyl ethers in complex small mols.

Science China: Chemistry published new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 52244-70-9 belongs to class ethers-buliding-blocks, and the molecular formula is C11H16O2, Electric Literature of 52244-70-9.

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

Noda, Hidetoshi; Asada, Yasuko; Shibasaki, Masakatsu published the artcile< O-Benzoylhydroxylamines as Alkyl Nitrene Precursors: Synthesis of Saturated N-Heterocycles from Primary Amines>, HPLC of Formula: 52244-70-9, the main research area is benzoylhydroxylamine alkyl nitrene precursor primary amine rhodium catalyst; synthesis saturated nitrogen heterocycle.

We introduce O-benzoylhydroxylamines as competent alkyl nitrene precursors. The combination of readily available, stable substrates and a proficient rhodium catalyst provides a straightforward means for the construction of various pyrrolidine rings from the corresponding primary amines. Preliminary mechanistic investigation suggests that the structure of the nitrene precursor plays a role in determining the nature of the resulting reactive intermediate.

Organic Letters published new progress about C-H bond activation. 52244-70-9 belongs to class ethers-buliding-blocks, and the molecular formula is C11H16O2, HPLC of Formula: 52244-70-9.

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

Cao, Wen-rui; Ge, Jing-qiu; Xie, Xin; Fan, Meng-lin; Fan, Xu-dong; Wang, Hong; Dong, Zhao-yue; Liao, Zhi-hua; Lan, Xiao-zhong; Chen, Min published the artcile< Protective effects of petroleum ether extracts of Herpetospermum caudigerum against α-naphthylisothiocyanate-induced acute cholestasis of rats>, HPLC of Formula: 52244-70-9, the main research area is Herpetospermum petroleum ether extract acute cholestasis alpha naphthylisothiocyanate; Acute cholestasis; Antioxidant; Herpetospermum caudigerum; Long-chain fatty acids; α-naphthylisothiocyanate.

The ripe seeds of Herpetospermum caudigerum have been used in Tibetan folk medicine for treatment of bile or liver diseases including jaundice, hepatitis, intumescences or inflammation. Previously reports suggested that the seed oil and some lignans from H. caudigerum exhibited protective effects against carbon tetrachloride (CCl4)-induced hepatic damage in rats, which may be related to their free radical scavenging effect. However, the protective effect of H. caudigerum against cholestasis is still not revealed. The aim of the present study was to investigate the pharmacol. effect and the chem. constituents of the petroleum ether extract (PEE) derived from H. caudigerum against α-naphthylisothiocyanate (ANIT)-induced acute cholestasis in rats. Male cholestatic Sprague-Dawley (SD) rats induced by ANIT (60 mg/kg) were orally administered with PEE (350, 700 and 1400 mg/kg). Levels of serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), alk. phosphatase (ALP), γ-Glutamyl transpeptidase (γ-GTP), total bilirubin (TBIL), direct bilirubin (DBIL) and total bile acid (TBA), as well as bile flow, and histopathol. assay were evaluated. Hepatic malondialdehyde (MDA), myeloperoxidase (MPO), superoxide dismutase (SOD), glutathione S-transferase (GST), and nitric monoxide (NO) in liver were measured to explore the possible protective mechanisms. Phytochem. anal. of PEE was performed by gas chromatog.-mass spectrometer (GC-MS). PEE have exhibited significant and dose-dependent protective effect on ANIT-induced liver injury by reduce the increases in serum levels of ALT, AST, ALP, γ-GTP, TBIL, DBIL and TBA, restore the bile flow in cholestatic rats, and reduce the severity of the pathol. tissue damage induced by ANIT. Hepatic MDA, MPO and NO contents in liver tissue were reduced, while SOD and GST activities were elevated in liver tissue. 49 compounds were detected and 39 of them were identified by GC-MS anal., in which long-chain fatty acids were the main constituents. PEE exhibited a dose-dependently protective effect on ANIT-induced liver injury in cholestatic rats with the potential mechanism of attenuated oxidative stress in the liver tissue, and the possible active compounds were long-chain fatty acids.

Journal of Ethnopharmacology published new progress about Bile acids Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 52244-70-9 belongs to class ethers-buliding-blocks, and the molecular formula is C11H16O2, HPLC of Formula: 52244-70-9.

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

Nuzzi, Andrea; Fiasella, Annalisa; Ortega, Jose Antonio; Pagliuca, Chiara; Ponzano, Stefano; Pizzirani, Daniela; Bertozzi, Sine Mandrup; Ottonello, Giuliana; Tarozzo, Glauco; Reggiani, Angelo; Bandiera, Tiziano; Bertozzi, Fabio; Piomelli, Daniele published the artcile< Potent α-amino-β-lactam carbamic acid ester as NAAA inhibitors. Synthesis and structure-activity relationship (SAR) studies>, Quality Control of 52244-70-9, the main research area is amino lactam carbamic acid ester acylethanolamine acid amidase inhibitor; Carbamates; Cysteine hydrolase; Inhibitors; N-acylethanolamine acid amidase; Structure–activity relationships; β-lactams.

4-Cyclohexylbutyl-N-[(S)-2-oxoazetidin-3-yl]carbamate I is a potent, selective and systemically active inhibitor of intracellular NAAA activity, which produces profound anti-inflammatory effects in animal models. In the present work, the authors describe structure-activity relationship (SAR) studies on 3-aminoazetidin-2-one derivatives, which have led to the identification of I, and expand these studies to elucidate the principal structural and stereochem. features needed to achieve effective NAAA inhibition. Investigations on the influence of the substitution at the β-position of the 2-oxo-3-azetidinyl ring as well as on the effect of size and shape of the carbamic acid ester side chain led to the discovery of II, a novel inhibitor of human NAAA that shows an improved physicochem. and drug-like profile relative to I. This favorable profile, along with the structural diversity of the carbamic acid chain of I, identify this compound as a promising new tool to investigate the potential of NAAA inhibitors as therapeutic agents for the treatment of pain and inflammation.

European Journal of Medicinal Chemistry published new progress about Anti-inflammatory agents. 52244-70-9 belongs to class ethers-buliding-blocks, and the molecular formula is C11H16O2, Quality Control of 52244-70-9.

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