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Heterocyclization reactions of ketene dithiolates

The reaction of ketene dithiolates in the presence of K2CO3 lead to bisthioalkylated products and thienothiophene derivatives depending on the strength of the base. The 1,5-diamino groups in thienothiophene compounds are subjected to heterocyclization under PTC conditions to get a variety of fused heterocycles.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Synthesis and reactivity of 2-chloro-5-(4-phenyl-1H-1,2,3-triazol-1-yl) benzenamine

The nucleophilic reactivity of 2-chloro-5-(4-phenyl-1H-1,2,3-triazol-1-yl) benzenamine 5 was studied with different reagents under ultrasonication.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Emergence through delicate balance between the steric factor and molecular orientation: a highly bright and photostable DNA marker for real-time monitoring of cell growth dynamics

Due to its remarkable structural and optical stability in biological milieu, a newly developed small molecule based DNA marker with high brightness (Phi = 0.51, brightness = 26?300 M?1 cm?1) and almost zero toxicity has been explored. For the first time to our knowledge, this approach has provided real-time monitoring of growth and reproductive potency of living cells beyond nine days.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters.

A series of novel benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters has been prepared. These compounds were tested as inhibitors of rat polymorphonuclear leukocyte 5-lipoxgenase (LO) in vitro and as inhibitors of leukotriene D4 (LTD4) and ovalbumin (OA) induced bronchospasm in the guinea pig (GP) in vivo. In general, inhibitory activity against 5-LO, LTD4, and OA was broadest for benzthiazole-containing analogues (benzthiazole greater than benzimidazole much greater than benzoxazole, benzofuran). The most potent 5-LO inhibitor, 4-[[3-(2-benzthiazolylmethoxy)-phenyl]hydroxyamino]-4-oxobutanoic acid methyl ester (7), had an IC50 of 0.36 microM. Compound 7, however, was inactive vs. OA. The most potent compound in vivo, 4-[[3-[(1-methyl-2-benzimidazolyl)methoxy]phenyl]-amino] -4-oxobutanoic acid methyl ester 4, inhibited both LTD4- and OA-induced bronchospasm by 83% and 60%, respectively, at 50 mg/kg intraduodenally. Compound 4 was studied in the Ames assay employing five strains of bacteria (TA1535, TA1537, TA1538, TA98, and TA100) with and without S-9 rat liver enzyme metabolic activation, and there was no significant number of reversions noted.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Dithiocarboxylic Acids, Dithiocarboxylic Esters, or Thiocarboxylic Amides by Reaction of Methylene-active Chloromethyl Compounds with Sulfur

With a mixture of sulfur and amine in DMF at room temperature halomethyl compounds (1,5-10) can be oxidized to give thiocarboxylic acids (2,11-16) and their derivatives (3,4,17-35).We studied this reaction in detail especially with chloroacetic derivatives (11-15) or chloromethyl heterocycles (16) formally derived from chloroacetic acid.The resulting thiooxalic acid derivatives (11-27) represent activated acids and very useful C2-synthons, especially for the synthesis of heterocycles.Oxidation in the presence of triethylamine leads to dithiocarboxylates (11-16) which can be alkylated to dithioesters (17-27) in high yields.As a rule, with different primary and secondary amines instead of tertiary amines these dithiocarboxylates or dithiocarboxylic esters can be transformed already at low temperatures to thioamides (28-35).

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Microwave-assisted alpha-halogenation of 2-methylquinolines with tetrabutylammonium iodide and 1,2-dichloroethane (1,2-dibromoethane)

A simple and efficient methodology permitting the halogenation of 2-methylquinolines into 2-(chloromethyl)quinolines or 2-(bromomethyl)quinolines in the tetrabutylammonium iodide and 1,2-dichloroethane (1,2-dibromoethane) system has been developed for the first time. The halogenation can be rapidly completed with good to excellent yields and high selectivity under microwave irradiation.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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1-AZA-BICYCLO [2.2.2] OCTANE DERIVATIVES USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS

The invention provides named compounds of formula (I), pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions and their use in therapy

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 4. 3-[2-(Benzoxazol-2-yl)ethyl]-5-ethyl-6- methylpyridin-2(1H)-one and analogues

A new series of potent specific 2-pyridinone reverse transcriptase (RT) inhibitors was developed based on the preliminary development lead 3- [(phthalimido)ethyl]-5-ethyl-6-methylpyridin-2(1H)-one (3), a non-nucleoside derivative which exhibited weak antiviral activity in cell culture against HIV-1 strain III(B). One compound, 3-[(benzoxazol-2-yl)ethyl]-5-ethyl-6- methylpyridin-2(1H)-one (9,L-696,229), which was a highly selective antagonist of the RT enzyme (IC50 = 23 nM) and which inhibited the spread of HIV-1 III(B) infection by >95% in MT4 human T-lymphoid cell culture (CIC95 = 50-100 nM), was selected for clinical evaluation as an antiviral agent.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Inhibitors of HIV reverse transcriptase

Novel pyridones inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Synthesis of Benzazolyl Pyrimidines Under Ultrasonication and Their Antimicrobial Activity

(1) The benzoxazolyl/benzothiazolyl/benzimidazolyl pyrimidines were prepared under ultrasonication in the presence of pyridine/dimethylaminopyridine and triethylamine. (2) Better yields were recorded in 4-(N,N-dimethylamino)pyridine and Et3N. (3) The presence of electron withdrawing chloro, bromo, and nitro substituents enhanced antimicrobial activity (13c, 13e, 14e: minimum inhibitory concentration?=?6.25?mug/well against Bacillus subtilis; 13e, 14e: minimum inhibitory concentration?=?6.25?mug/well against Aspergillus niger).

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Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem