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An environmentally benign procedure for the synthesis of substituted 2-thiobenzothiazoles, 2-thiobenzoxazoles, 2-thiobenzimidazoles, and 1,3-oxazolopyridine-2-thiols

An improved environmentally benign procedure for the synthesis of substituted 2-thio-benzothia(oxa)zoles, 2-thiobenzimidazoles, and 1,3-oxazolopyridine-2-thiols by cyclization of 2-aminophenols, 2-aminothiophenols, 1,2-phenylenediamines, or 2-amino-3-hydroxypyridines with potassium O-ethyldithiocarbonate in PEG 400 or glycerol under directed microwave irradiation is described. The method can be applied to the synthesis of a variety of derivatives. Springer-Verlag 2011.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Benzoxazoline and benzimidazoline derivatives as novel aldose reductase inhibitors, part 2: Lead optimization

We designed novel aldose reductase inhibitors, benzoxazoline and benzimidazoline derivatives, based on lead evolution from spiroquinazolinones. In order to optimize in vivo activity in the lens, variously substituted derivatives were synthesized. The relationship between structure and in vitro activity was also analyzed by comparative molecular field analysis. The optimized compound exhibited high potency in the lens.

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Benzoxazole – Wikipedia,
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5-chloro-2 – [5 – (R)-methyl -1,4-diazepan-1 -] phenyltheophylline diozaiole method for the preparation of (by machine translation)

The invention relates to 5-chloro-2 – [5 – (R)-methyl -1,4-diazepan-1 -] phenyltheophylline diozaiole method for preparing, the method comprising reducing the compound of formula I the step of shows. The invention also relates to new shown in formula I the intermediate compound. 5-chloro-2 – [5 – (R)-methyl -1,4-diazepan-1 -] phenyltheophylline diozaiole used for the treatment of sleep disorders is an important intermediate for pharmaceutical Suvorexant. The preparation method of this invention from an initial raw material is introduced to the chiral center, in the process of the whole reaction, the reaction with chiral center will be affected and reagent, avoid the chiral resolution or chiral catalyst, the cost is high, the method of low yield, the participation of there are no chiral in process reaction, the chiral purity of the product, only by using a conventional method and apparatus, the operation is simple, mild condition, route is short, high yield, is suitable for industrial production. (by machine translation)

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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2-azolylmethyl-2-phenyl-4-[benzazol-2-yloxy-or-thio-methyl]-1,3 dioxolanes and salts thereof, pharmaceutical compositions containing them and their use

Compounds of the formula I STR1 and the acid-addition salts thereof, where A=CH or N; Ar=naphthyl, thienyl or phenyl; Z=oxygen or sulfur; R1 =alkyl, F or Cl; g=0-2; L=0 or 1; m=0-4; p=0 or 1; X=O, S or N–R3 ; R2 =alkyl, alkoxy, halogen, SCH3, COC6 H5, CF3, COOCH3, COOC2 H5, or NO2 ; n=0-2; R2, under certain circumstances, is alternatively –CH=CH–CH=CH– or phenoxy are described. Processes for the preparation thereof are also described. Compounds IIIa STR2 are valuable intermediates for the preparation of I. The compounds I serve as antimycotics.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Synthesis and anticancer activity evaluation of N-[4-(2-methylthiazol-4-yl) phenyl]acetamide derivatives containing (benz)azole moiety

A new class of novel thiazole-(benz)azole derivatives was synthesized to investigate their anticancer activity. The structure of the compounds was confirmed by IR, 1H-NMR, and MS spectral data and elemental analyses. Anticancer effect of the compounds was evaluated against A549 and C6 tumor cell lines. MTT, analysis of DNA synthesis, acridine orange/ethidium bromide staining method and analysis of caspase-3 activation assays were performed for anticancer activity investigations. Compounds 6f and 6g, which carry 5-chloro and 5-methylbenzimidazole groups showed significant anticancer activity. Potential of these compounds to direct tumor cells to apoptotic pathway, which is a precondition of anticancer action, was also observed.

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Benzoxazole – Wikipedia,
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Electric Literature of 4570-41-6, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.4570-41-6, Name is Benzo[d]oxazol-2-amine, molecular formula is C7H6N2O. In a article£¬once mentioned of 4570-41-6

Metal-Free Synthesis of Thiosulfonates via Insertion of Sulfur Dioxide

A simple and catalyst-free strategy was developed for the synthesis of unsymmetrical thiosulfonates using readily available DABCO?(SO2)2 as a solid and bench-stable sulfur dioxide surrogate. The corresponding thiosulfonates were obtained through a radical pathway with good functional group tolerance. This strategy offers a promising synthesis method for the construction of diverse and useful thiosulfonates in the field of synthetic and pharmaceutical chemistry and extends the number of still limited sulfur dioxide fixation strategies. (Figure presented.).

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

The Absolute Best Science Experiment for 4570-41-6

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Electric Literature of 4570-41-6, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.4570-41-6, Name is Benzo[d]oxazol-2-amine, molecular formula is C7H6N2O. In a Article£¬once mentioned of 4570-41-6

Green Approach for the Synthesis of a New Class of Diamidomethane-linked Benzazolyl Pyrazoles and Evaluation as Antifungals

A new class of diamidomethane-linked benzoxazolyl pyrazoles, benzothiazolyl pyrazoles, and benzimidazolyl pyrazoles were synthesized from the synthetic intermediates N-benzazolylcarbamoylmethylcinnamides adopting environmentally benign methods. In fact, nitrile imine was generated from araldehyde phenylhydrazone in the presence of iodosobenzene and cetyltrimethylammonium bromide followed by oxidation with iodine in dimethylsulfoxide. The structures of compounds were characterized by IR, 1H NMR, 13C NMR, and mass spectra. The title compounds were also evaluated for their antifungal activity. Amongst all the tested compounds benzimidazolyl pyrazolyl carboxamides (13a and 13b) were found to be potential antifungal agents.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Reference of 151230-42-1, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 151230-42-1, molcular formula is C8H6BrNO, introducing its new discovery.

Fluorescent dye and preparation method and application thereof (by machine translation)

The invention belongs to the technical field of organic synthesis, and particularly relates to a fluorescent dye and a preparation method and application. The structural general formula of the fluorescent dye is shown in formula I in the specification, wherein X and Y are the same or different O, S, C (CH). 3 )2 Or NR6 , R2 And R3 R is hydrogen or functional group identical or different, R1 , R4 , R5 And R6 Both functional groups, Z. The anion. The fluorescent dye has a living cell membrane permeability, can be used for fluorescence imaging of living cell microstructures, and can acquire fluorescence imaging such as living cell STED super-resolution fluorescence imaging and laser confocal focusing. (by machine translation)

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 16707-41-8, name is 1-(4-(Benzo[d]oxazol-2-yl)phenyl)-1H-pyrrole-2,5-dione, introducing its new discovery. Product Details of 16707-41-8

METHODS FOR PROMOTING MOTOR NEURON SURVIVAL

The present invention relates to methods for promoting motor neuron survival, treating or preventing neurodegenerative disorders, identifying agents that promote survival of motor neurons, identifying agents that are useful for treating neurodegenerative disorders, diagnosing neurodegenerative disorders, predicting the progression of a neurodegenerative disorder in a subject, and monitoring the effectiveness of a therapy in reducing the progression of a neurodegenerative disorder in a subject.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Development of small-molecule Trypanosoma brucei N-myristoyltransferase inhibitors: Discovery and optimisation of a novel binding mode

The enzyme N-myristoyltransferase (NMT) from Trypanosoma brucei has been validated both chemically and biologically as a potential drug target for human African trypanosomiasis. We previously reported the development of some very potent compounds based around a pyrazole sulfonamide series, derived from a high-throughput screen. Herein we describe work around thiazolidinone and benzomorpholine scaffolds that were also identified in the screen. An X-ray crystal structure of the thiazolidinone hit in Leishmania major NMT showed the compound bound in the previously reported active site, utilising a novel binding mode. This provides potential for further optimisation. The benzomorpholinone was also found to bind in a similar region. Using an X-ray crystallography/structure-based design approach, the benzomorpholinone series was further optimised, increasing activity against T. brucei NMT by >1000-fold. A series of trypanocidal compounds were identified with suitable in vitro DMPK properties, including CNS exposure for further development. Further work is required to increase selectivity over the human NMT isoform and activity against T. brucei. HATs off to diversity! Screening a diverse library against Trypanosoma brucei N-myristoyltransferase (NMT) identified hits based on thiazolidinone and benzomorpholine scaffolds. X-ray crystallography of these compounds bound to Leishmania major NMT revealed novel active site binding conformations. Using the structural information, the benzomorpholine scaffold was optimised to a blood-brain barrier penetrant compound with activity against TbNMT of <0.002 mum. Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.SDS of cas: 41014-43-1, you can also check out more blogs about41014-43-1

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem