Category: 22876-22-8

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AlCl3-Promoted Synthesis of 2-Mercapto Benzoheterocycles by Using Sodium Dimethyldithiocarbamate as Thiocarbonyl Surrogate

A simple, expeditious and high-efficiency synthetic method for the AlCl3-mediated one-pot preparation of 2-mercapto benzoheterocycles (2-mercapto benzothiazoles, benzoxazoles and benzimidazoles) is described. By the treatment of a series of S, O and N heteroatoms containing bifunctional molecules with sodium dimethyldithiocarbamate in AlCl3, the desired benzoheterocycles are obtained smoothly. The protocol can also be applied on the synthesis of a series of thiazolidine-2-thiones, imidazolidine-2-thiones. This novel synthetic approach has advantages such as ligand-free, high efficiency, short reaction time, readily available starting materials and simple experimental procedures.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Recommanded Product: 22876-22-8, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 22876-22-8, name is 5-Methylbenzo[d]oxazole-2(3H)-thione. In an article£¬Which mentioned a new discovery about 22876-22-8

Selective synthesis of 2-aminobenzoxazoles and 2-mercaptobenzoxazoles by using o-aminophenols as starting material

2-Aminobenzoxazoles and 2-mercaptobenzoxazoles were selectively synthesized by treating o-aminophenols with dithiocarbamates and tetramethylthiuram disulfide (TMTD), respectively. With the promotion of NaH/CuI, the reaction of o-aminophenols with dithiocarbamates gave 2-aminobenzoxazoles with good yield (70?92%) in one pot manner, and 2-mercaptobenzoxazoles were synthesized (yield: 55?80%) in the presence of K2CO3 by treating o-aminophenols with tetramethylthiuram disulfide (TMTD). The feature of this method includes good to excellent yield, easy performance and broad substrate scope, which makes the protocol practical and attractive in the preparation of some potential pharmaceutically active compounds.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Synthesis and analgesic activities of some 2-(benzazolylacetyl)amino-3- ethoxycarbonylthiophene derivatives

In this study, some 2-[2-(benzazole-2-thioxy)acetylamino]-3- ethoxycarbonylthiophene and 2-[2-(benzazole-1-yl)acetylamino]-3- ethoxycarbonylthiophene compounds were obtained by the reaction of 2-chloroacetylamino-3-ethoxycarbonylthiophene derivatives and a suitable benzazole-2-thione or benzimidazole derivatives. Analgesic activities of the compounds were tested by using tail-flick and tail-immersion methods. It is reported that some of the compounds showed remarkable analgesic activities. Copyright Taylor & Francis Inc.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Synthesis of some 2-[(benzazole-2-yl)Thio]-diphenylmethylacetamide derivatives and their antimicrobial activity

Some 2-[(benzazole-2-yl)thio]diphenylmethylacetamide derivatives were synthesized by reacting 2-chloroacethylaminodiphenylmethane with benzazole-2-thions. The structure elucidation of the compounds was performed by IR, 1H NMR, and MS-FAB spectral data. Antimicrobial activity of the compounds was examined. Some of the compounds have shown similar antifungal activities against C. albicans when compared with ketoconazole. It was also observed that some of these compounds have moderate antimicrobial activity when compared with chloramphenicole.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Product Details of 22876-22-8, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 22876-22-8, name is 5-Methylbenzo[d]oxazole-2(3H)-thione. In an article£¬Which mentioned a new discovery about 22876-22-8

STUDIES ON HETEROCYCLIC COMPOUNDS. XXXIV. SYNTHESIS OF 2-SUBSTITUTED AMINOBENZOXAZOLES WITH NICKEL PEROXIDE

Oxidation of N-methyl (or phenyl)-N’-(4-methylpyrid-2-yl)thiourea (Ia, b) with nickel peroxide (Ni-PO) under reflux in benzene or acetonitrile afforded the corresponding ureas (IIa, b).N-(2-Hydroxy-5-methylphenyl)-N’-methylthiourea (IVa) was synthesized by the reaction of 2-amino-4-methylphenol (III) and methyl isothiocyanate in benzene under reflux.Howevwer, the reaction of III and phenyl isothiocyanate in benzene under reflux did not afford the thiourea (IVb) but IVb was obtained in ethanol at room temperature.NiPO oxidation of thioureas (IVa-f) in acetonitrile at room temperature afforded 2-substituted aminobenzoxazoles (VIIa-f) in good yields.The reaction mechanisms of Ni-PO and thioureas (Ia, b and IVa-f) are discussed.Keywords: – N-substituted N’-(4-methylpyrid-2-yl)thioureas; N-substituted N’-(4-methylpyrid-2-yl)ureas; N-(2-hydroxyphenyl) N’-substituted thioureas; 2-substituted aminobenzoxazoles; nickel peroxide; oxidative cyclization; 2-mercaptobenzoxazole; isothiocyanates

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, name: 5-Methylbenzo[d]oxazole-2(3H)-thione, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 22876-22-8, Name is 5-Methylbenzo[d]oxazole-2(3H)-thione, molecular formula is C8H7NOS

Design, synthesis, molecular docking, and anticancer activity of benzoxazole derivatives as VEGFR-2 inhibitors

Novel series of benzoxazoles 4a-f-16 were designed, synthesized, and evaluated for anticancer activity against HepG2, HCT-116, and MCF-7 cells. HCT-116 was the most sensitive cell line to the influence of the new derivatives. In particular, compound 5e was found to be the most potent against HepG2, HCT-116, and MCF-7 with IC50 = 4.13 ¡À 0.2, 6.93 ¡À 0.3, and 8.67 ¡À 0.5 muM, respectively. Compounds 5c, 5f, 6b, 5d, and 6c showed the highest anticancer activities against HepG2 cells with IC50 of 5.93 ¡À 0.2, 6.58 ¡À 0.4, 8.10 ¡À 0.7, 8.75 ¡À 0.7, and 9.95 ¡À 0.9 muM, respectively; HCT-116 cells with IC50 of 7.14 ¡À 0.4, 9.10 ¡À 0.8, 7.91 ¡À 0.6, 9.52 ¡À 0.5, and 12.48 ¡À 1.1 muM, respectively; and MCF-7 cells with IC50 of 8.93 ¡À 0.6, 10.11 ¡À 0.9, 12.31 ¡À 1.0, 9.95 ¡À 0.8, and 15.70 ¡À 1.4 muM, respectively, compared with sorafenib as a reference drug with IC50 of 9.18 ¡À 0.6, 5.47 ¡À 0.3, and 7.26 ¡À 0.3 muM, respectively. The most active compounds 5c-f and 6b,c were further evaluated for their vascular endothelial growth factor receptor-2 (VEGFR-2) inhibition. Compounds 5e and 5c potently inhibited VEGFR-2 at lower IC50 values of 0.07 ¡À 0.01 and 0.08 ¡À 0.01 muM, respectively, compared with sorafenib (IC50 = 0.1 ¡À 0.02 muM). Compound 5f potently inhibited VEGFR-2 at low IC50 value (0.10 ¡À 0.02 muM) equipotent to sorafenib. Our design was based on the essential pharmacophoric features of the VEGFR-2 inhibitor sorafenib. Molecular docking was performed for all compounds to assess their binding pattern and affinity toward the VEGFR-2 active site.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Based on 1, 3 – propanedithiol as mercapto source synthesis 2 – oxa (thia) and mercaptobenzothiazole azole compound of preparation method (by machine translation)

The invention belongs to the field of medical and chemical intermediate synthesis, provides a based on 1, 3 – propanedithiol as mercapto source synthesis 2 – oxa (thia) and mercaptobenzothiazole azole compound of preparation method, under protection of inert gas, in dimethyl sulfoxide solvent, the oxa (thia) substituted azole with 1, 3 – propanedithiol in the presence of a alkali 120 – 140 C heating and stirring, reaction 12 – 24 hours later, the reaction is cooled down to room temperature, after the acidification is carried out processing to obtain the product. The invention has the reaction condition is simple, functional group compatibility advantages of better and higher yield; the prepared 2 – mercapto-benzoxazole and 2 – mercaptobenzothiazole compound is an important organic synthetic intermediates, raw material in the chemical industry, pesticide, medicine and other field has a very wide application, has strong practical value and social and economic benefits. (by machine translation)

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Benzoxazole – Wikipedia,
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Application of 22876-22-8, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, and a compound is mentioned, 22876-22-8, 5-Methylbenzo[d]oxazole-2(3H)-thione, introducing its new discovery.

Synthesis of some 2-[(benzazole-2-yl)thioacetylamino]thiazole derivatives and their antimicrobial activity and toxicity

Some 2-[(benzazole-2-yl)thioacetylamino]thiazole derivatives (III) were synthesized by reacting 4-methyl-2-(chloroacetylamino)thiazole derivatives (I) with benzazol-2-thiole (II) in acetone in the presence of K2CO 3. The chemical structures of the compounds were elucidated by 1H NMR and FAB+-MS spectral data. The prepared compounds were tested for antimicrobial activity and toxicity.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Regioselective thiolation of arenes and heteroarenes: C-H functionalization strategy for C-S bond formation

A facile transition-metal-free oxidative cross-dehydrogenative coupling reaction involving selective formation of a C-S bond leading to the synthesis of arylthiobenzoxazoles, heteroarylthiobenzoxazoles, and arylthiobenzothiazoles has been described. This highly regioselective C-H functionalization reaction with electron-rich aromatic systems including heteroaromatics is achieved by reversing the reactivity of sulfur in the presence of a suitable oxidant and strong acid. (Chemical Equation Presented).

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

22876-22-8, Name is 5-Methylbenzo[d]oxazole-2(3H)-thione, belongs to benzoxazole compound, is a common compound. Recommanded Product: 5-Methylbenzo[d]oxazole-2(3H)-thioneIn an article, once mentioned the new application about 22876-22-8.

Benzoxazolamines and Benzothiazolamines: Potent, Enantioselective Inhibitors of Leukotriene Biosynthesis with a Novel Mechanism of Action

A series of benzoxazolamine and benzothiazolamine analogs that inhibit leukotriene (LT) biosynthesis are described.The initial lead, (S)-N-(benzothiazol-2-yl)phenylalanine ethyl ester (5a), was discovered in a screening program for inhibition of Ca-ionophore-A23187-induced LTB4 release in human polymorphonuclear leukocytes (IC50 0.23 muM).Through structural modification, it was determined that hydrophobic substituents in the 5-position and replacement of the phenyl ring of phenylalanine with a cyclohexyl group greatly enhance potency.Several ester bioisosteres that retain potency and enantiomeric selectivity are described.Lead optimization culminated in (S)-N-<2-cyclohexyl-1-(2-pyridinyl)ethyl>-5-methyl-2-benzoxazolamine (43b), IC50 0.001 muM.The compounds described are not inhibitors of 5-lipoxygenase but, rather, act at the level of arachidonic acid release.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem