Month: December 2022

Timofeeva, Maria N. published the artcileTuning the Catalytic Performance of Novel Composites Based on ZIF-8 and Nafen through Dimensional and Concentration Effects in the Synthesis of Propylene Glycol Methyl Ether, Related Products of ethers-buliding-blocks, the publication is European Journal of Organic Chemistry (2019), 2019(26), 4215-4225, database is CAplus.

Zeolitic imidazolate framework (ZIF-8, Zn(2-meIm)₂) and composites based on ZIF-8 and alumina nanofibers (Nafen^TM), i.e. ZIF-8/Nafen, were demonstrated to be efficient heterogeneous catalysts for the reaction of methanol with propylene oxide to produce propylene glycol Me ether (PGME), which is a member of the family of glycol ether solvents used for a wide variety of consumer products and industrial applications. Both the reaction rate and the selectivity toward PGME were found to decrease with increasing crystal size of the ZIF-8 material, which was related to the change in the number of basic sites and their accessibility. The investigation of ZIF-8/Nafen composites revealed the dependence of their catalytic performance on the amount of the ZIF-8 component. In particular, the activity was affected by the crystal size of the ZIF-8 material and the nature of acid-base sites in its framework.

European Journal of Organic Chemistry published new progress about 1589-47-5. 1589-47-5 belongs to ethers-buliding-blocks, auxiliary class Aliphatic hydrocarbon chain,Alcohol,Ether, name is 2-Methoxypropan-1-ol, and the molecular formula is C6H9N3, Related Products of ethers-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Jacquesy, Rose published the artcileIsomerization and oxidation of simple ketones in superacid medium, Related Products of ethers-buliding-blocks, the publication is Bulletin de la Societe Chimique de France (1978), 255-62, database is CAplus.

Treatment of cyclohexanones having a tertiary C α or β to the CO group, e.g., carvomenthone (I, R = Me, Z = O, Z¹ = H₂), menthone(I, R = Me, Z = H₂, Z¹ = O), I (R = H, Z = H₂ Z¹ =O) with HF-SbF₅ gave the isomerization, ring contraction, or dehydrogenation derivatives, e.g., II (R¹-R⁴ = Me, Et, Me, H; H, Me, H,CHMe₂), III, IV (R⁵-R⁸ = H, CH₂CHMe₂, H, Me; Me, CHMe₂, Me, H; H, Me H, CHMe₂ via protonation of the O whereas 3-methyl- and 3,3,5-trimethylcyclohexanone did not react with the acids. However, in cyclohexenones, dehydrogenation occurred only if the product was stable, e.g., V (R⁹ = H, R¹⁰ = CHMe₂) dehydrogenated with HF-SbF₅ to give the conjugated VI whereas with V (R⁹ = R¹⁰ = Me; R⁹ = H, R¹⁰ = Et) no dehydrogenation products were obtained.

Bulletin de la Societe Chimique de France published new progress about 2944-47-0. 2944-47-0 belongs to ethers-buliding-blocks, auxiliary class Benzene,Ether, name is 2-Isopropylanisole, and the molecular formula is C10H14O, Related Products of ethers-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Young, Trudye A. published the artcileA pramoxine-based anti-itch lotion is more effective than a control lotion for the treatment of uremic pruritus in adult hemodialysis patients, COA of Formula: C17H28ClNO3, the publication is Journal of Dermatological Treatment (2009), 20(2), 76-81, database is CAplus and MEDLINE.

Objective: The objective of this study was to evaluate the efficacy of a com. available anti-itch lotion containing 1% pramoxine hydrochloride vs. control lotion in the treatment of uremic pruritus in adult hemodialysis patients. Methods: This was a randomized, double-blind, controlled comparative trial set in a community hemodialysis center. The study population comprised 28 individuals (mean age 53.5) with moderate to severe uremic pruritus who had been receiving hemodialysis for at least 3 mo. All participants were recruited from one community hemodialysis center. Topical anti-itch lotion containing 1% pramoxine was applied twice daily to all affected areas of pruritus for 4 wk. The main outcome measure was a reduction in itch intensity. Secondary outcomes included increases in the investigator’s global assessment and improvement in skin hydration. Results: There was a 61% decrease in itch intensity in the treatment group, whereas a 12% reduction in itch intensity was observed in the control group. The rate of decline in itching was also greater in the treatment arm vs. the control arm. No significant differences were displayed in other studied disease-related variables. Conclusion: Our study shows that individuals using pramoxine 1% lotion experienced a reduction in pruritus to a greater degree than those using the control lotion. This safe, convenient and effective topical lotion may potentially benefit the large number of patients affected by pruritus associated with end-stage renal disease.

Journal of Dermatological Treatment published new progress about 637-58-1. 637-58-1 belongs to ethers-buliding-blocks, auxiliary class Inhibitor, name is 4-(3-(4-Butoxyphenoxy)propyl)morpholine hydrochloride, and the molecular formula is C6H17NO3Si, COA of Formula: C17H28ClNO3.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Lele, S. S. published the artcileCyanocoumarins, Name: 2-Methoxyacetamide, the publication is Journal of Organic Chemistry (1962), 637-9, database is CAplus.

Some cyanocoumarins were prepared by the Rosenmund-von Braun reaction on the halogenated coumarin in order to study their hydrolysis. The iodo derivative (0.01 mol) was mixed with 0.02 mol anhydrous CuCN, heated at the specified temperature 10 min., the mixture powd., extracted with either Me₂CO or AcOH, and the residue from the extract recrystallized from AcOH (needles). Addition of cyano derivative from a previous run to the mixture gave a higher yield. The following cyanocoumarins were thus obtained (coumarin, Rosenmund-von Braun reaction temperature, m.p., and % yield given): 7-methoxy-8-cyano, 180-90°, 269-70°, 60; 7-methoxy-3-cyano, 180-90°, 225-30°, 40; 7-methoxy-8-cyano-6-carbomethoxy, 210-20°, 102°, 54; 7-methoxy-8-cyano-4-carbomethoxymethyl, 190-210°, 192°, 22; 7-methoxy-8-cyano-4-Me, 220-30°, 289-91°, 55; 7-methoxy-3-cyano-4-Me, 180-5°, 223°, 75; 7-methoxy-8-cyano-4-methyl-6-carbomethoxy, 240-5°, 276°, 70; 7-methoxy-3-cyano-4-methyl-6-carbomethoxy, 250-5°, 249°, 70; 5-methoxy-8-cyano-4-Me, 260-70° 227-30° 46; 5-methoxy-8-cyano-4-methyl-6-carbomethoxy, 225-30° 236° 44. Hydrolysis A. The eyano compound (0.5 g.) was heated 2-3 h. with 90% H₂SO₄, the solid obtained on pouring the mixture on ice extracted with dilute NaHCO₃, and the product crystallized from AcOH. Method B. The cyanocoumarin (0.5 g.) was heated 2-3 h. with 10% alc. KOH, the product acidified, purified through NaHCO₃, and crystallized from AcOH. The following hydrolysis products from the cyanocoumarins mentioned above were obtained (hydrolysis method, product obtained, and m.p. given): A, 7-methoxy-8-carbamoyl, 277-9°; A, 7-methoxy-8-carbamoyl-6-carboxy, 267-8°; B, 7-methoxy8-cyano-6-carboxy, 228°; A, 7-methoxy-8-carbamoyl-4-acetic acid, 235-8°; B, 7-methoxy-8-cyano-4-acetic acid, 274-5° (and 7-methoxy-8-cyano-4-Me, -); A, 7-methoxy-8-carbamoyl-4-Me, 278°; A and B, 7-methoxy-4-methyl-3-carboxy, 184-5°; A, 7-methoxv-8-carbamoyl-4methyl-6-carboxy, 272°; B, 7-methoxy-8-cyano-4-methyl-6carboxy, 283°; A, 7-methoxy-4-methyl-3,6-dicarboxy, 20810°; B, 7-methoxy-3-cyano-4-methyl-6-carboxy, 248°; A, 5-methoxy-8-carbamoyl-4-Me, 286°; A, 5-methoxy-8carbamoyl-4-methyl-6-carboxy, 272°; B, 5-methoxy-8-cyano-4-methyl-6-carboxy, 248°. The carbamoyl derivative (0.5 g.) heated 3 h. at 120° with 18 mL. 50% H₂SO₄ and the mixture poured on ice gave the following results (method of hydrolysis, coumarin product obtained, m.p. given): III, 7-hydroxy-8-carboxy, 230°; 10% alkali or 50% H₂SO₄, 7-methoxy-6-carboxyl,-; 10% alkali or 50% H₂SO₄, 7-methoxy-4-Me, -; 10% alkali or 50% H₂SO₄, 7-methoxy-4methyl-8-carboxy, -; 10% alkali or 50% H₂SO₄, 7-methoxy-4-methyl-6-carboxy, -; 50% H₂SO₄, 5-methoxy-4-methyl-8-carboxy, 286°; 50% H₂SO₄, 5-methoxy-4-methyl-6,8-dicarboxy, 284°. The methoxycyanocoumarin was dissolved in Ac₂O, heated 3 h. with HI at 120°, and the product crystallized from AcOH. The following hydroxycyanocoumarins were thus obtained (coumarin and m.p. given): 7hydroxy-8-cyano, 305°; 7-hydroxy-8-cyano-4-Me, 272°; 7-hydroxy-3-cyano-4-Me, 298°; 5-hydroxy-8-cyano-4-Me, 276°.

Journal of Organic Chemistry published new progress about 16332-06-2. 16332-06-2 belongs to ethers-buliding-blocks, auxiliary class Amine,Aliphatic hydrocarbon chain,Amide,Ether, name is 2-Methoxyacetamide, and the molecular formula is C3H7NO2, Name: 2-Methoxyacetamide.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Kanhed, Ashish M. published the artcileIndoloquinoxaline derivatives as promising multi-functional anti-Alzheimer agents, Application In Synthesis of 6850-57-3, the publication is Journal of Biomolecular Structure and Dynamics (2022), 40(6), 2498-2515, database is CAplus and MEDLINE.

To confront a disease like Alzheimer’s disease having complex pathogenesis, development of multitarget-directed ligands has emerged as a promising drug discovery approach. In our endeavor towards the development of multitarget-directed ligands for Alzheimer’s disease, a series of indoloquinoxaline derivatives were designed and synthesized. In vitro cholinesterase inhibition studies revealed that all the synthesized compounds exhibited moderate to good cholinesterase inhibitory activity. 6-(6-(Piperidin-1-yl)hexyl)-6H-indolo[2,3-b]quinoxaline was identified as the most potent and selective BuChE inhibitor (IC₅₀ = 0.96μM, selectivity index = 0.17) that possessed 2 fold higher BuChE inhibitory activity compared to the com. approved reference drug donepezil (IC₅₀ = 1.87μM). Moreover, compound is also endowed with self-induced Aβ1-42 aggregation inhibitory activity (51.24% inhibition at 50μM concentration). Some of the compounds of the series also displayed moderate anti-oxidant activity. To perceive a putative binding mode of the compound, mol. docking studies were carried out, and the results pointed out significant interactions of compound with the enzymes in the binding sites of cholinesterases as well as Aβ1-42. Addnl., compound exhibited favorable in silico ADMET properties. Put together these findings project compound as a potential multitarget-directed ligand in the direction of developing novel anti-AD drugs.Communicated by Ramaswamy H.

Journal of Biomolecular Structure and Dynamics published new progress about 6850-57-3. 6850-57-3 belongs to ethers-buliding-blocks, auxiliary class Amine,Benzene,Ether, name is (2-Methoxyphenyl)methanamine, and the molecular formula is C8H11NO, Application In Synthesis of 6850-57-3.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Bompart, Jacques published the artcileSynthesis of new β-blocking analogs of bevantolol, SDS of cas: 2944-47-0, the publication is Annales Pharmaceutiques Francaises (1985), 42(6), 537-45, database is CAplus.

The 9 bevantolol analogs I (R¹ = OMe, Cl, OPh, SMe, CHMe₂; R² = OH, Cl, OMe, OPh, SMe, CHMe₂) were prepared None of the compounds showed activity comparable to that of propranolol when tested for inhibition of isoprenaline-induced tachycardia and hypotension in dogs.

Annales Pharmaceutiques Francaises published new progress about 2944-47-0. 2944-47-0 belongs to ethers-buliding-blocks, auxiliary class Benzene,Ether, name is 2-Isopropylanisole, and the molecular formula is C10H14O, SDS of cas: 2944-47-0.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Schuster, Ingeborg I. published the artcileEnhancement of the resonance interaction of out-of-plane methoxy groups by ortho-substituents in crowded anisoles, COA of Formula: C10H14O, the publication is Journal of Organic Chemistry (1988), 53(25), 5819-25, database is CAplus.

The ¹⁷O and ¹³C NMR chem. shifts of substituted anisoles provide evidence that the resonance interaction of methoxy groups which are perpendicular to the aromatic ring in crowded anisoles is influenced, to varying degrees, by ortho substituents. Enhancement of methoxy-to-aryl electron delocalization, brought about by these groups, follows the order isopropyl < ethyl < methyl << methoxy (in-plane) < tert-Bu. By an anal. of the mol. structures of several 3,5-dialkylanisic acids, related to 2,6-dialkylanisoles, this order becomes explicable in terms of repulsions between the lone pair electrons of the methoxy oxygen and bonding electrons of the proximate substituents. Methoxy groups that lie in the mol. plane are not similarly affected by neighboring substituents.

Journal of Organic Chemistry published new progress about 2944-47-0. 2944-47-0 belongs to ethers-buliding-blocks, auxiliary class Benzene,Ether, name is 2-Isopropylanisole, and the molecular formula is C24H12, COA of Formula: C10H14O.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Ruan, Zheming published the artcileSubstituted diaryl ether compounds as retinoic acid-related orphan Receptor-γt (RORγt) agonists, SDS of cas: 2944-47-0, the publication is Bioorganic & Medicinal Chemistry Letters (2021), 127778, database is CAplus and MEDLINE.

The discovery of a series of substituted diarylether compounds as retinoic acid related orphan receptor γt (RORγt) agonists is described. Compound 1 was identified from deck mining as a RORγt agonist. Hit-to-lead optimization led to the identification of lead compound 5, which possesses improved potency (10x). Extensive SAR exploration led to the identification of a potent and selective compound 22, that demonstrated an improved pharmacokinetic profile and a dose-dependent pharmacodynamic response. However, when dosed in a MC38 syngeneic tumor model, no evidence of efficacy was observed

Bioorganic & Medicinal Chemistry Letters published new progress about 2944-47-0. 2944-47-0 belongs to ethers-buliding-blocks, auxiliary class Benzene,Ether, name is 2-Isopropylanisole, and the molecular formula is C10H14O, SDS of cas: 2944-47-0.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Rajendiran, Senkuttuvan published the artcileIonic-Liquid-Based Heterogeneous Covalent Triazine Framework Cobalt Catalyst for the Direct Synthesis of Methyl 3-Hydroxybutyrate from Propylene Oxide, Recommanded Product: 2-Methoxypropan-1-ol, the publication is Inorganic Chemistry (2017), 56(12), 7270-7277, database is CAplus and MEDLINE.

β-Hydroxy esters are considered as potential building blocks for the production of fine chems. and potential drug mols. in various industries. Developing an efficient and recyclable catalyst for the synthesis of β-hydroxy esters is challenging. Here we report the first ionic-liquid-based heterogenized cobalt catalyst, [imidazolium-CTF][Co(CO)₄], for the direct ring-opening carbonylation of propylene oxide to Me 3-hydroxybutyrate (MHB) with 86% selectivity (>99% conversion).

Inorganic Chemistry published new progress about 1589-47-5. 1589-47-5 belongs to ethers-buliding-blocks, auxiliary class Aliphatic hydrocarbon chain,Alcohol,Ether, name is 2-Methoxypropan-1-ol, and the molecular formula is C4H10O2, Recommanded Product: 2-Methoxypropan-1-ol.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Garland, Keira published the artcileOptimization of globomycin analogs as novel gram-negative antibiotics, COA of Formula: C25H23NO4, the publication is Bioorganic & Medicinal Chemistry Letters (2020), 30(20), 127419, database is CAplus and MEDLINE.

Discovery of novel classes of Gram-neg. antibiotics with activity against multi-drug resistant infections is a critical unmet need. As an essential member of the lipoprotein biosynthetic pathway, lipoprotein signal peptidase II (LspA) is an attractive target for antibacterial drug discovery, with the natural product inhibitor globomycin offering a modestly-active starting point. Informed by structure-based design, the globomycin depsipeptide was optimized to improve activity against E. coli. Backbone modifications, together with adjustment of physicochem. properties, afforded potent compounds with good in vivo pharmacokinetic profiles. Optimized compounds such as (I) (E. coli MIC 3.1μM) and (II) (E. coli MIC 0.78μM) demonstrate broad spectrum activity against gram-neg. pathogens and may provide opportunities for future antibiotic discovery.

Bioorganic & Medicinal Chemistry Letters published new progress about 77128-73-5. 77128-73-5 belongs to ethers-buliding-blocks, auxiliary class Inhibitor, name is (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)(methyl)amino)-3-phenylpropanoic acid, and the molecular formula is C25H23NO4, COA of Formula: C25H23NO4.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem