Archives for Chemistry Experiments of 2879-20-1

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In a fresh approach to the synthesis of N-vinylazoles, a ligand-free palladium catalytic system was found to promote the Csp2-N bond-forming reaction utilizing N-tosylhydrazones and N-H azoles. This process shows functional group tolerance; di-, tri-, and tetrasubstituted N-vinylazoles were obtained in high yields. Under the optimized conditions, the reaction proceeds with high stereoselectivity depending on the nature of the coupling partners.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

New explortion of C10H10O3

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Styrene-acrylic acid compound and its preparation and use in medicine (by machine translation)

The invention discloses a novel benzene propanoic acid compound represented by formula I, an optical isomer and a raceme thereof as well as physiologically acceptable salts, a solvate and a crystallizing form thereof. The invention further discloses a preparation method of the compound, a medicine preparation containing the compound and a clinical application of the compound for treating diseases related to insulin resistance.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Solution phase synthesis of a spiro[pyrrolidine-2,3′-oxindole] library via a three component 1,3-dipolar cycloaddition reaction

A combinatorial library of 26,500 spiro[pyrrolidine,-2,3-oxindoles] was prepared in a single-compound format by a facile intermolecular 1,3-dipolar cycloaddition. An azomethine ylide, generated by the decarboxylative condensation of an isatin 1 with an alpha-amino acid 2, was trapped by a transchalcone 3 to afford heterocycles of the general structure 4. The regio- and stereochemistry of a representative product was determined by single crystal X-ray structure.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Extracurricular laboratory:new discovery of C10H10O3

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Chalcone?benzoxaborole hybrids as novel anticancer agents

In this study, we report the synthesis of a series of chalcone?benzoxaborole hybrid molecules and the evaluation of their anticancer activity. Their anticancer potency and toxicity were tested on three human cancer cell lines and two normal cell lines. The 4-fluoro compound 15 was found to be the most potent compound with an IC50value of 1.4 muM on SKOV3 cells. The 4-iodo compound 18 and 3-methyloxy-4-amino compound 47 showed good potency on SKOV3 cells while exhibiting low toxicity on normal cells. This work extended the application of benzoxaboroles to the field of anticancer research.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Final Thoughts on Chemistry for C10H10O3

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In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. HPLC of Formula: C10H10O3, 2879-20-1, name is 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone. In an article,Which mentioned a new discovery about 2879-20-1

Pyrrolidine-3-carboxylic acids as endothelin antagonists. 2. Sulfonamide-based ET(A)/ET(B) mixed antagonists

When the N,N-dialkylacetamide side chain of the highly ET(A)-selective endothelin antagonist ABT-627 (1; [2R,3R,4S]-2-(4-methoxyphenyl)-4-(1,3- benzodioxol-5-yl)-1-[[(N,N-dibutylamino)carbonyl]methyl]pyrrolidine-3- carboxylic acid; A-147627) is replaced by N,S-dialkylsulfonami-doethyl, the resultant analogs retain ET(A) affinity, but exhibit substantial ET(B) affinity as well. Structure-activity studies reveal that modifications in the length of the two alkyl groups, and in the substitution on the anisyl ring, are important in optimizing this ‘balanced’ antagonist profile. In particular the combination of an N-n-propyl group, an S-alkyl chain between four and six carbons in length, and a fluorine atom ortho to the aromatic OCH3 provides compounds with sub-nanomolar affinities for both receptor subtypes, and with ET(A)/ET(B) ratios close to 1. A number of these compounds also exhibit oral bioavailabilities (in rats) in the 30-50% range and have substantial plasma half-lives. The balanced receptor-binding profile of these potent and orally bioavailable compounds complements the ET(A) selectivity observed with 1.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Synthesis of quaternary 8-(1-acylethene-1-yl)-13-methylcoptisine chlorides and their selective growth inhibitory activity between human cancer cell lines and normal intestinal epithelial cell-6

In this paper, quaternary 8-(1-acylethene-1-yl)-13-methylcoptisine chlorides targeting thioredoxin reductases (TrxRs) were designed to test the growth inhibitory activity against human cancer cell lines and the effect on viability of the normal intestinal epithelial cell-6 (IEC-6) in vitro and to evaluate structure-activity relationship (SAR). The introduced alpha beta-unsaturated ketone groups at C-8 consisting of n-alkanoyls possessing five to ten carbons or aroyls or cyclohexylcarbonyl increased the tested activity against the target cancer cell lines. By and large, this type of improvement was increasingly graced by the elongation of the aliphatic chain of the n-alkanoyls in the range of less than ten carbon atoms. The relatively more polar 1-acylethene-1-yls displayed no effect on improving the activity. All the explored aroyls showed significant effect on improving the activity of the target compounds against the tested cancer cell lines with no SAR being observed. The findings of this study suggested that oil/water partition coefficient of the test compounds was one of the key factors impacting the target activity against the tested cancer cell lines. At the concentration of 10 mumol/L, except for the compounds with n-alkanoyls possessing seven or more carbons or with alpha-naphthoyl, none of the other compounds displayed obvious cytotoxicity on normal IEC-6 cell when co-incubated. The survival rate of IEC-6 cell ranged from 75% to 100% for the noncytotoxic compounds.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Diketo acids and their amino acid/dipeptidic analogues as promising scaffolds for the development of bacterial methionine aminopeptidase inhibitors

Using diketoesters as the template, various derivatives were designed and the selected compounds were synthesized as bacterial methionine aminopeptidase (MetAP) inhibitors. The results of in vitro antibacterial screening revealed fifteen compounds (1a-c, 1e-h, 1j, 1l, 2a-c, 3d, 5c and 5e) as potent against different bacterial strains. By using the MTT assay on human cell line (HepG2), the viability of cell proliferation was evaluated and nine compounds (1c, 1e, 1j, 1l, 2a,b, 3d, 5c and 5e) showed no cytotoxic effect at the concentration range of 50-450 mug ml-1. In the biochemical evaluation against methionine aminopeptidase (MetAPs) from Streptococcus pneumonia (SpMetAP), Mycobacterium tuberculosis (MtMetAP), Enterococcus faecalis (EfMetAP) and human (HsMetAP), compounds displayed differential behaviour against these four enzymes. Moreover, compound 1g showed 84% inhibition of SpMetAP, while compound 3d selectively inhibited MtMetAP with 79% inhibition and little effect on HsMetAP at 100 muM concentration. At the same concentration, compound 5e exhibited 87% and 85% inhibition of EfMetAP and SpMetAP, respectively. Understanding the mode of binding through modeling at the active site provided the structural basis for the possible mode of inhibition. Together, these data will be useful for further development of diketo acid based inhibitors with improved potency and selectivity.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Archives for Chemistry Experiments of C10H10O3

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Target-oriented synthesis: Miscellaneous synthetic routes to access 1,4-enediones through the coupling of 1,3-dicarbonyl compounds with multiform substrates

Target-oriented synthetic protocol was presented for the synthesis of 1,4-enediones. The approach can efficiently construct 1,4-enediones through different reaction pathways from multiform substrates alpha-halo aromatic ketones, 2-hydroxy-aromatic ketones and methyl carbinols. In this reaction, CuI was found to be the most efficient catalyst. Multiform substrates were also found to perform well to afford the products in a one-pot fashion.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Solid-phase synthesis of 3-aryl-3-oxo-propan amides by reaction of lithium enolates with 4-nitrophenyl carbamate resin or polymer-bound isocyanate

Two synthetic procedures to enable a straightforward and efficient solid-phase synthesis of 3-aryl-3-oxo-propan amides (beta-keto amides) are described and compared. Lithium enolates, which can be obtained by deprotonation of methyl ketones with LiHMDS, are added to either an immobilized isocyanate or activated carbamate. After cleavage of the products from the solid support, various 3-aryl-3-oxo-propan amides are released in high yield and purity. The advantage of this method is that many of the commercially available methyl ketone building blocks can be used. The immobilized 3-aryl-3-oxo-propan amides generated may serve as intermediates for the preparation of structurally diverse libraries.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 2879-20-1

Related Products of 2879-20-1, In homogeneous catalysis, catalysts are in the same phase as the reactants. Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. In a document type is Article, and a compound is mentioned, CAS :2879-20-1, Name is 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone, introducing its new discovery.

Formation of N-alkylpyrroles via intermolecular redox amination

(Chemical Equation Presented) A wide variety of aldehydes, ketones, and lactols undergo redox amination when allowed to react with 3-pyrroline in the presence of a mild Bronsted acid catalyst. This reaction utilizes the inherent reducing power of 3-pyrroline to perform the equivalent of a reductive amination to form alkyl pyrroles. In doing so, the reaction avoids stoichiometric reducing agents that are typically associated with reductive aminations. Moreover, the redox amination protocol allows access to alkyl pyrroles that cannot be made via standard reductive amination.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem