Month: December 2022

Andrews, Jonathan A. published the artcileSulfinates from Amines: A Radical Approach to Alkyl Sulfonyl Derivatives via Donor-Acceptor Activation of Pyridinium Salts, Quality Control of 6850-57-3, the publication is Organic Letters (2021), 23(21), 8488-8493, database is CAplus and MEDLINE.

Synthetically versatile alkyl sulfinates RSO₂R¹ (R = cyclobutyl, Bn, pyridin-2-ylmethyl, etc.; R¹ = F, 2-(tert-butoxy)-2-oxoethyl, Ph, Bn, etc.) can be prepared from readily available amines RNH₂, using Katritzky pyridinium salt intermediates I. In a catalyst-free procedure, primary, secondary, and benzylic alkyl radicals are generated by photoinduced or thermally induced single-electron transfer (SET) from an electron donor-acceptor (EDA) complex, and trapped by SO₂ to generate sulfonyl radicals. Hydrogen atom transfer (HAT) from Hantzsch ester gives alkyl sulfinate products, which are used to prepare a selection of medicinal chem. relevant sulfonyl-containing motifs.

Organic Letters 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, Quality Control of 6850-57-3.

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

Keiser, Jennifer published the artcileEvaluation of an FDA approved library against laboratory models of human intestinal nematode infections, Related Products of ethers-buliding-blocks, the publication is Parasites & Vectors (2016), 376/1-376/10, database is CAplus and MEDLINE.

Background: Treatment options for infections with soil-transmitted helminths (STH) – Ascaris lumbricoides, Trichuris trichiura and the two hookworm species, Ancylostoma duodenale and Necator americanus – are limited despite their considerable global health burden. The aim of the present study was to test the activity of an openly available FDA library against laboratory models of human intestinal nematode infections. Methods: All 1,600 drugs were first screened against Ancylostoma ceylanicum third-stage larvae (L3). Active compounds were scrutinized and toxic compounds, drugs indicated solely for topical use, and already well-studied anthelmintics were excluded. The remaining hit compounds were tested in parallel against Trichuris muris first-stage larvae (L1), Heligmosomoides polygyrus third-stage larvae (L3), and adult stages of the three species in vitro. In vivo studies were performed in the H. polygyrus and T. muris mice models. Results: Fifty-four of the 1,600 compounds tested revealed an activity of > 60% against A. ceylanicum L3 (hit rate of 3.4%), following incubation at 200μM for 72 h. Twelve compounds progressed into further screens. Adult A. ceylanicum were the least affected (1/12 compounds active at 50μM), while eight of the 12 test compounds revealed activity against T. muris L1 (100μM) and adults (50μM), and H. polygyrus L3 (200μM). Trichlorfon was the only compound active against all stages of A. ceylanicum, H. polygyrus and T. muris. In addition, trichlorfon achieved high worm burden reductions of 80.1 and 98.9%, following a single oral dose of 200 mg/kg in the T. muris and H. polygyrus mouse model, resp. Conclusion: Drug screening on the larval stages of intestinal parasitic nematodes is feasible using small libraries and important given the empty drug discovery and development pipeline for STH infections. Differences and commonalities in drug activities across the different STH species and stages were confirmed. Hits identified might serve as a starting point for drug discovery for STH.

Parasites & Vectors 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 C17H28ClNO3, Related Products of ethers-buliding-blocks.

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

Pasieka, Anna published the artcileDiscovery of multifunctional anti-Alzheimer’s agents with a unique mechanism of action including inhibition of the enzyme butyrylcholinesterase and γ-aminobutyric acid transporters, Recommanded Product: (2-Methoxyphenyl)methanamine, the publication is European Journal of Medicinal Chemistry (2021), 113397, database is CAplus and MEDLINE.

Looking for an effective anti-Alzheimer’s agent is very challenging; however, a multifunctional ligand strategy may be a promising solution for the treatment of this complex disease. We herein present the design, synthesis and biol. evaluation of novel hydroxyethylamine derivatives displaying unique, multiple properties that have not been previously reported. The original mechanism of action combines inhibitory activity against disease-modifying targets: β-secretase enzyme (BACE1) and amyloid β (Aβ) aggregation, along with an effect on targets associated with symptom relief – inhibition of butyrylcholinesterase (BuChE) and γ-aminobutyric acid transporters (GATs). Among the obtained mols., compound 36 (I) exhibited the most balanced and broad activity profile (eeAChE IC₅₀ = 2.86μM; eqBuChE IC₅₀ = 60 nM; hBuChE IC₅₀ = 20 nM; hBACE1 IC₅₀ = 5.9μM; inhibition of Aβ aggregation = 57.9% at 10μM; mGAT1 IC₅₀ = 10.96μM; and mGAT2 IC₅₀ = 19.05μM). Moreover, we also identified 31 (II) as the most potent mGAT4 and hGAT3 inhibitor (IC₅₀ = 5.01μM and IC₅₀ = 2.95μM, resp.), with high selectivity over other subtypes. Compounds 36 and 31 represent new anti-Alzheimer agents that can ameliorate cognitive decline and modify the progress of disease.

European Journal of Medicinal Chemistry 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, Recommanded Product: (2-Methoxyphenyl)methanamine.

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

Bortolami, Martina published the artcileDesign, synthesis and biological evaluation of a series of iron and copper chelating deferiprone derivatives as new agents active against Candida albicans, SDS of cas: 6850-57-3, the publication is Bioorganic & Medicinal Chemistry Letters (2021), 128087, database is CAplus and MEDLINE.

Candida albicans, in specific conditions, is responsible of severe invasive systemic candidiasis that are related to its ability to produce biofilm on biol. and artificial surfaces. Many studies reported the role of iron in fungal growth and virulence and the ability of metal chelating agents to interfere with C. albicans metabolism, virulence and biofilm formation. Here we report the activity of 3-hydroxy-1,2-dimethyl-4(1H)-pyridinone (deferiprone) derivatives against C. albicans planktonic cells and biofilm. Some of the studied compounds (2b and 3b) were able to chelate Fe(III) and Cu(II), and showed an interesting activity on planktonic cells (MIC50 of 32μg/mL and 16μg/mL resp.) and on biofilm formation (BMIC50 of 32μg/mL and 16μg/mL resp.) in cultured ATCC 10,231C. albicans; this activity was reduced, in a concentration dependent way, by the addition of Fe(III) and Cu(II) to the culture media. Furthermore, the most active compound 3b showed a low toxicity on Galleria mellonella larvae.

Bioorganic & Medicinal Chemistry Letters 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, SDS of cas: 6850-57-3.

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

Donthireddy, S. N. R. published the artcile[(PPh₃)₂NiCl₂]-Catalyzed C-N Bond Formation Reaction via Borrowing Hydrogen Strategy: Access to Diverse Secondary Amines and Quinolines, Recommanded Product: N-(4-Methoxybenzyl)pyridin-2-amine, the publication is Journal of Organic Chemistry (2021), 86(9), 6994-7001, database is CAplus and MEDLINE.

Com. available [(PPh₃)₂NiCl₂] was found to be an efficient catalyst for the mono-N-alkylation of (hetero)aromatic amines, employing alcs. to deliver diverse secondary amines, including the drug intermediates chloropyramine and mepyramine in excellent yields (up to 97%) via the borrowing hydrogen strategy. This method shows a superior activity (TON up to 10000) with a broad substrate scope at a low catalyst loading of 1 mol % and a short reaction time. Further, this strategy was also successful in accessing various quinoline derivatives following the acceptorless dehydrogenation pathway.

Journal of Organic Chemistry published new progress about 52818-63-0. 52818-63-0 belongs to ethers-buliding-blocks, auxiliary class Pyridine,Amine,Benzene,Ether, name is N-(4-Methoxybenzyl)pyridin-2-amine, and the molecular formula is C13H14N2O, Recommanded Product: N-(4-Methoxybenzyl)pyridin-2-amine.

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

Timofeeva, M. N. published the artcileSynthesis of propylene glycol methyl ether from methanol and propylene oxide over alumina-pillared clays, Application of 2-Methoxypropan-1-ol, the publication is Applied Catalysis, B: Environmental (2011), 102(3-4), 433-440, database is CAplus.

Al-pillared interlayered clays (Al-PILCs) were synthesized by the exchange reaction between Na-clay and Al-hydroxypolycation solutions aged for 0.5-14 days and characterized by DRS-UV-vis, x-ray diffraction, FT-IR and N₂-adsorption/desorption analyses, Hammett acidity titration with n-butylamine and FT-IR spectroscopy using PhCN and CDCl₃ as probe mols. The aging time of Al-hydroxypolycation pillaring solution affects both the textural characteristics and the physicochem. properties of Al-PILCs. Al-PILCs were tested as catalysts for synthesis of propylene glycol Me ether from methanol and propylene oxide. Increase in Al content due to the prolonged aging time favors the increase in the activity of Al-PILCs.

Applied Catalysis, B: Environmental 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 C4H6O3, Application of 2-Methoxypropan-1-ol.

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

Timofeeva, M. N. published the artcileEffect of the acid-base properties of Zr,Al-pillared clays on the catalytic performances in the reaction of propylene oxide with methanol, Synthetic Route of 1589-47-5, the publication is Applied Catalysis, B: Environmental (2011), 104(1-2), 54-63, database is CAplus.

A series of Zr,Al-pillared interlayered clays (Zr,Al-PILCs) have been prepared and characterized by X-ray diffraction, elemental anal., FT-IR and N2-adsorption/desorption analyses, 27Al NMR(MAS), FT-IR spectroscopy using pyridine, PhCN and CDCl3 as probe mols. It was found that textural and physicochem. properties of Zr,Al-PILCs depend on Zr content in clay. The relationship between the acid-base properties and catalytic performances of Zr,Al-PILCs was revealed in the synthesis of propylene glycol Me ether from methanol and propylene oxide. The results show that the conversion of propylene oxide and the selectivity to 1-methoxy-2-propanol decrease with increasing the amount of zirconium in Zr,Al-PILCs due to the change in acid-base properties.

Applied Catalysis, B: Environmental 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 C20H19NO4, Synthetic Route of 1589-47-5.

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

Wang, Xue Chao published the artcileA new method for synthesis of o-isopropyl substituted aromatic compounds, Application In Synthesis of 2944-47-0, the publication is Chinese Chemical Letters (1992), 3(5), 329-32, database is CAplus.

Heteroatom-directed aromatic lithiation reactions used for the regiospecific synthesis of o-iso-Pr substituted phenolic and benzyl alc. compounds are described. Thus, lithiation of, e.g., PhOMe or PhCH₂OH with BuLi in THF followed by treatment with Me₂CO gave alcs. which on dehydration with H₂SO₄ containing a catalytic amount of p-toluenesulfonic acid followed by hydrogenation over Raney Ni gave desired compounds, e.g., 76% 2-Me₂CHC₆H₄OMe and 61% 2-Me₂CHC₆H₄CH₂OH, resp.

Chinese Chemical 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 C42H63O3P, Application In Synthesis of 2944-47-0.

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

Pang, Sujuan published the artcileComponent analysis of poly propylene carbonate washing liquid in washing section, Quality Control of 1589-47-5, the publication is Huaxue Fenxi Jiliang (2012), 21(4), 34-36, database is CAplus.

Washing liquid of the poly propylene carbonate in washing section was analyzed qual. and quant. by gas chromatog. mass spectrometry. The results showed that the main impurities of washing liquid were 1-methoxyl-2-propanol, 2-methoxyl-1-propanol, methyl-carbonate, dipropylene glycol, propylene carbonate. The mass fraction of propylene epoxide and methanol in the first washing liquid was 32.34% and 58.74%, in the fourth washing liquid were 10.61% and 89.01% resp. With the washing time increasing, the methanol content increased and the propylene epoxide content reduced.

Huaxue Fenxi Jiliang 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, Quality Control of 1589-47-5.

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

Shi, Tiancai published the artcileMatrix effect compensation for analyte protectants during aroma component analysis of tobacco, Application of 2-Methoxynaphthalene, the publication is Yancao Keji (2021), 54(9), 27-39, database is CAplus.

In order to solve the challenge that strong polar analyte protectants are not well performed in weak polar solvent systems, the solution of acetonitrile:dichloromethane = 2:1 (V/V) was chosen as weak polarity solvent system. The effects of 23 compounds as analyte protectants on the heights and shapes of chromatog. peaks of 31 aroma components were investigated. The chromatog. peaks of the aroma components in solvent added with these analyte protectants were compared with those in tobacco matrix. After optimizing the type, composition and concentration of the protectants, a suitable combination of analyte protectants was developed. In addition, 15 aroma components in tobacco (other than the 31 aroma components mentioned above) were chosen to verify the matrix compensation effect of the developed analyte protectant combination. The results showed that the suitable analyte protectants combination was malic acid (1000 mg/L) + 1,2-tetradecanediol (1000 mg/L). By adding the optimized analyte protectants combination into the solvent standard solution, a satisfactory matrix compensation effect was achieved. The linearity of the calibration curve for each aroma component was greatly improved, and the slope and linear correlation coefficient (r²) were basically consistent with the matrix-matched calibration curve. The matrix effect of aroma components in tobacco during GC/MS anal. was compensated by adding analyte protectants.

Yancao Keji published new progress about 93-04-9. 93-04-9 belongs to ethers-buliding-blocks, auxiliary class Naphthalene,Ether, name is 2-Methoxynaphthalene, and the molecular formula is C11H10N4, Application of 2-Methoxynaphthalene.

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