Discovery of 5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one

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NEW LOW SIDE EFFECT PHARMACEUTICAL COMPOSITION CONTAINING ANTITUBERCULOSIS DRUGS

A pharmaceutical composition for treating tuberculotic diseases with no side effect/low side effect is provided by the present invention, which pharmaceutically effective amount of one or more compounds chosen from isoniazid, rifampin, pyrazinamide and ethambutol, and pharmaceutically effective amount of substances which can reduce the side effect of the antituberculosis agents.

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Properties and Exciting Facts About 2-Oxo-2,3-dihydrobenzo[d]oxazole-6-carboxylic acid

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NEW BENZOYL UREA DERIVATIVES

The new benzoyl urea derivatives of formula (I) wherein the meaning of X and Y independently are hydrogen atom, hydroxy, benzyloxy, amino, nitro, C1-C4 alkylsulfonamido optionally substituted with a halogen atom or halogen atoms, C1-C4 alkanoylamido optionally substituted with a halogen atom or halogen atoms, C1-C4 alkoxy, aroyl-carbamoyl optionally substituted with halogen atom or C1-C4 alkyl or C1-C4 alkoxycarbonyl group, or the neighboring X and Y groups optionally form together with one or more identical or different additional hetero atom and-CH= and/or-CH2-groups an optionally substituted 4-7 membered homo-or heterocyclic ring, preferably morpholine, pyrrole, pyrrolidine, oxo-or thioxo-pyrrolidine, pyrazole, pyrazolidine, imidazole, imidazolidine, oxo-or thioxo-imidazole or imidazolidine, 1,4-oxazine, oxazole, oxazolidine, triazole, oxo-or thioxo-oxazolidine, or 3-oxo-l,4-oxazine ring, V and Z independently are hydrogen or halogen atom, cyano, C1-C 4 alkyl, C1-C4 alkoxy, trifluoromethyl, hydroxy or optionally esterized carboxyl group, W is oxygen atom, as well as C1-C4 alkylene, C2-C4 alkenylene, aminocarbonyl,-NH-,-N(alkyl)-,-CH2O-,-CH 2S-,-CH(OH)-,-OCH2-group, wherein the meaning of alkyl is a C1-C4 alkyl group-, when the dotted bonds ( — ) represent simple C-C bonds then U is hydroxy group or hydrogen atom or when W is C1-C4 alkylene or C2-C4 alkenylene group, then one of the dotted bonds ( — ) can represent a further double C-C bond and in this case U means an electron pair, which participate in the double bond and optical antipodes, racemates and the salts thereof are highly effective and selective antagonists of NMDA receptor, and moreover most of the compounds are selective antagonist of NR2B subtype of NMDA receptor. Furthermore objects of the present invention are the pharmaceutical compositions containing new benzoyl urea derivatives of formula (I) or optical antipodes or racemates or the salts thereof as active ingredients and processes for producing these compounds and pharmaceutical compositions.

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More research is needed about 4570-41-6

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Progress in the synthesis of 2-aminobenzoxazole derivatives

2-Aminobenzoxazole derivatives are a kind of heterocyclic compounds, which play important roles in medicine, biology and material science, and their synthetic methods have attracted much attention. In recent years, many efficient, green synthetic approaches of 2-aminobenzoxazole derivatives using transition-metal or metal-free catalytic systems have been reported. Based on differences of reaction substrates and synthetic methods, the recent advances in the synthesis of 2-aminobenzoxazole derivatives are reviewed.

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Some scientific research about 2-Methylbenzo[d]oxazol-6-amine

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Acetamide and substituted acetamide-containing thiourea inhibitors of herpes viruses

Compounds of the formula: are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.

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Awesome and Easy Science Experiments about Benzo[d]oxazol-2-amine

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Efficient transposition of the sandmeyer reaction from batch to continuous process

The transposition of Sandmeyer chlorination from a batch to a safe continuous-flow process was investigated. Our initial approach was to develop a cascade method using flow chemistry which involved the generation of a diazonium salt and its quenching with copper chloride. To achieve this safe continuous process diazotation, a chemometric approach (Simplex method) was used and extrapolated to establish a fully continuous-flow method. The reaction scope was also examined via the synthesis of several (het)aryl chlorides. Validation and scale-up of the process were also performed. A higher productivity was obtained with increased safety.

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Extended knowledge of 5-Nitro-2,3-dihydro-1,3-benzoxazol-2-one

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2, 4 -DIAMINOPYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS

The present invention relates to novel pyrimide derivatives of formula (I): that are useful as kinase inhibitors. More particularly, the present invention relates to novel pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders

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Top Picks: new discover of 22876-21-7

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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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Can You Really Do Chemisty Experiments About 1-(Benzo[d]oxazol-2-yl)ethanone

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Assembling heterocycle-tethered C-glycosyl and alpha-amino acid residues via 1,3-dipolar cycloaddition reactions

(Equation Presented) The 1,3-dipolar cycloadditions of C-glycosyl nitrile oxides and acetylenes to an alkyne and an azide, respectively, bearing a masked glycinyl moiety furnished disubstituted isoxazoles and triazoles. Unveiling the glycinyl group in these cycloadducts afforded C-glycosyl alpha-amino acids in which the two bioactive entities were tethered through rigid five-membered heterocycles. Optimized entries to the same compounds involved the use of unmasked but protected alkyne- and azide-containing amino acids as the partners of 1,3-dipolar cycloadditions.

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Awesome Chemistry Experiments For 5-Nitro-2,3-dihydro-1,3-benzoxazol-2-one

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The vicarious nucleophilic substitution of hydrogen and related reactions in nitrobenzoxazoles

5- and 6-nitrobenzoxazoles 3 and 4 react with nucleophiles exclusively at C-2, giving ring opening products. If position 2- is blocked with phenyl substituent the reaction takes place in the carbocyclic ring affording the VNS products. 2-Methylthio-5-nitrobenzoxazole 7 and its 6-nitro isomer 8 give products which result from addition of a nucleophile to the carbocyclic ring (VNS) as well as to the heterocyclic ring (S(N)Ar and ring cleavage). 2-Methylthiobenzoxazoles can be readily converted to the corresponding benzoxazolones via oxidative hydrolysis.

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Discovery of Benzo[d]oxazol-2-amine

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Rhodium-Catalyzed Chemo-, Regio-, and Enantioselective Allylation of 2-Aminothiazoles with Terminal Allenes

A rhodium-catalyzed chemo-, regio- and enantioselective intermolecular coupling reaction of 2-aminobenzothiazoles with terminal allenes is reported. The new reaction displays a wide substrate scope for both reaction partners to deliver the allylation products in good yields, with excellent regio- and enantioselectivity. This novel methodology was further applied in an efficient synthesis of chiral isothiourea.

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