Heterocyclic Building Blocks-Benzisoxazole

In an article, author is Chimichi, Stefano, once mentioned the application of 532-32-1, Name: Sodium benzoate, Name is Sodium benzoate, molecular formula is C7H5NaO2, molecular weight is 144.1032, MDL number is MFCD00012463, category is Benzisoxazole. Now introduce a scientific discovery about this category.

First example of diels-alder reaction of 4-(1-ethenylsubstituted)-3-methylisoxazoles with acetylenedicarboxylates

The first example of a [4+2] cycloaddition reaction of 4-(1-ethenylsubstituted)isoxazoles with acetylenedicarboxylates is reported, while the corresponding 5-substituted isomers do not react with the same dienophile; density functional theory (DFT) calculation indicate the electronic origin of the different behaviour.

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Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Application of 298-12-4, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 298-12-4, Name is 2-Oxoacetic acid, SMILES is OC(=O)C=O, belongs to Benzisoxazole compound. In a article, author is WEPPLO, P, introduce new discover of the category.

5-ARYLOXYBENZISOXAZOLE ESTERS – SYNTHESIS AND HERBICIDAL ACTIVITY

A series of benzisoxazole glycolate and acetate ester diphenyl ethers were prepared. The preparation of intermediate 5-hydroxybenzisoxazoleacetic acid from 4,6-dihydroxycoumarin was improved by reaction in the presence of excess hydroxylamine hydrochloride. The resultant diphenyl ether herbicides were potent total vegetation control pre- and postemergence herbicides.

Application of 298-12-4, Because enzymes can increase reaction rates by enormous factors and tend to be very specific, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 298-12-4.

Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. Recommanded Product: 3,3-Dimethyl-2-oxobutanoic acid, 815-17-8, Name is 3,3-Dimethyl-2-oxobutanoic acid, SMILES is CC(C)(C)C(C(O)=O)=O, in an article , author is MAKOSZA, M, once mentioned of 815-17-8.

DOES NITROARYLATION OF PHENYLACETONITRILE PROCEED AS A PHASE-TRANSFER-CATALYZED PROCESS

The phase-transfer catalyzed reaction of phenylacetonitrile with 4-chloro-3-(trifluoromethyl)nitrobenzene produces 5-chloro-7-phenyl-4-(trifluoromethyl)benzisoxazole (5) not the nitroarylation product 3a as was reported by Durantini et al. (Durantini, E. N.; Chiacchiera, S. M.; Silber, J. J. J. Org. Chem. 1993, 58, 7115). The catalytic nitroarylation does not occur because the product 3a immediately forms a lipophilic carbanion which inhibits the catalytic process. The nitroarylation occurs under ion-pair extraction conditions when a stoichiometric amount of tetrabutylammonium bromide is used, whereas 2-phenylalkanenitriles are efficiently PTC nitroarylated. 4-Chloro-3-(trifluoromethyl)- and 2-chloro-5-(trifluoromethyl)nitrobenzenes enter vicarious nucleophilic substitution reactions with carbanions of chloromethyl p-tolyl sulfone. These results and formation of 5 show that carbanions add to these nitroarenes initially in positions occupied with hydrogen.

But sometimes, even after several years of basic chemistry education, it is not easy to form a clear picture on how they govern reactivity! 815-17-8, you can contact me at any time and look forward to more communication. Recommanded Product: 3,3-Dimethyl-2-oxobutanoic acid.

Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Chemistry, like all the natural sciences, begins with the direct observation of nature¡ª in this case, of matter.625-08-1, Name is 3-Hydroxy-3-methylbutanoic acid, SMILES is CC(C)(O)CC(O)=O, belongs to Benzisoxazole compound. In a document, author is Panza, Francesco, introduce the new discover, Recommanded Product: 625-08-1.

Pharmacological management of dementia with Lewy bodies with a focus on zonisamide for treating parkinsonism

Introduction Dementia with Lewy bodies (DLB) has no approved symptomatic or disease-modifying treatments in the US and Europe, despite being the second most common cause of neurodegenerative dementia. Areas covered Herein, the authors briefly review the DLB drug development pipeline, providing a summary of the current pharmacological intervention studies. They then focus on the anticonvulsant zonisamide, a benzisoxazole derivative with a sulfonamide group and look at its value for treating parkinsonism in DLB. Expert opinion Several new compounds are being tested in DLB, the most innovative being those aimed at decreasing brain accumulation of alpha-synuclein. Unfortunately, new drug testing is challenging in terms of consistent diagnostic criteria and lack of reliable biomarkers. Few randomized controlled trials (RCTs) are well-designed, with enough power to detect significant drug effects. Levodopa monotherapy can treat the parkinsonism in DLB, but it can cause agitation or visual hallucination worsening. Two Phase II/III RCTs of DLB patients recently reported a statistically significant improvement in motor function in those receiving zonisamide as an adjunctive treatment to levodopa. New biomarker strategies and validated outcome measures for DLB or prodromal DLB may enhance clinical trial design for the development of specific disease-modifying treatments.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 625-08-1 is helpful to your research. Recommanded Product: 625-08-1.

Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

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, Product Details of 815-17-8, 815-17-8, Name is 3,3-Dimethyl-2-oxobutanoic acid, SMILES is CC(C)(C)C(C(O)=O)=O, belongs to Benzisoxazole compound. In a document, author is Chaker, Aida, introduce the new discover.

New 3-substituted-2,1-benzisoxazoles: Synthesis and antimicrobial activities

A new series of 3-substituted-2,1-benzisoxazoles (anthranils) were prepared by different methods and characterized by spectroscopic methods and mass spectrometry. These 2,1-benzisoxazoles were tested in vitro for their antiplasmodial activity on a chloroquine-resistant strain of Plasmodium falciparum (P.f.) (FcB1), and for antimicrobial activity against representative bacterial and fungal strains, as well as for cytotoxicity on MCF7 human breast cancer cells. Given the log P-calc and selectivity index values (cytotoxicity/antiplasmodial activity ratio), the benzo[c] isoxazol-3- ylmethylene-phenyl-amine (11) (imino-benzisoxazole) was identified as the best hit against P.f. (FcB1), and the benzo[c] isoxazol-3-yl-phenyl-methanone (3) (3-acyl-2,1-benzisoxazole) against P.f. and the Geotrichum candidum fungal strain. (c) 2013 Production and hosting by Elsevier B.V. on behalf of King Saud University.

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 815-17-8. Product Details of 815-17-8.

Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds. 35963-20-3, Name is ((1R,4S)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonic acid, molecular formula is C10H16O4S, belongs to Benzisoxazole compound, is a common compound. In a patnet, author is Falch, E, once mentioned the new application about 35963-20-3, COA of Formula: C10H16O4S.

Selective inhibitors of glial GABA uptake: Synthesis, absolute stereochemistry, and pharmacology of the enantiomers of 3-hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazole (exo-THPO) and analogues

3-Methoxy-4,5,6,7-tetrahydro-1,2-benzisoxazol-4-one (20a), or the corresponding 3-ethoxy analogue (20b), and 3-chloro-4,5,6,7-tetrahydro-1,2-benzisothiazol-4-one (51) were synthesized by regioselective chromic acid oxidation of the respective bicyclic tetrahydrobenzenes 19a,b and 50, and they were used as key intermediates for the syntheses of the target; zwitterionic 3-isoxazolols 8-15 and 3-isothiazolols 16 and 17, respectively. These reaction sequences involved different reductive processes. Whereas (RS)-4-amino-3-hydroxy-4,5,6,7-tetrahydro-1,2-benzisoxazole (8, exo-THPO) was synthesized via aluminum amalgam reduction of oxime 22a or 22b, compounds 9,11-13, and 15-17 were obtained via reductive aminations. Compound 10 was synthesized via N-ethylation of the N-Boc-protected primary amine 25. The enantiomers of 8 were obtained in high enantiomeric purities (ee greater than or equal to 99.1%) via the diastereomeric amides 32 and 33, synthesized from the primary amine 23b and (R)-alpha-methoxyphenylacetyl chloride and subsequent separation by preparative HPLC. The enantiomers of 9 were prepared analogously from the secondary amine 27. On the basis of X-ray crystallographic analyses, the configuration of oxime 22a was shown to be E and the absolute configurations of (-)-8 . HCl and (+)-9 . HBr were established to be R. The effects of the target compounds on GABA uptake mechanisms in vitro were measured using a rat brain synaptosomal preparation and primary cultures of mouse cortical neurons and glia cells (astrocytes). Whereas the classical GABA uptake inhibitor, (R)-nipecotic acid (2), nonselectively inhibits neuronal (IC50 = 12 mu M) and glial (IC50 = 16 mu M) GABA uptake and 4,5,6,7-tetrahydroisoxazolo[4,5-c]pyridin-3-ol (1, THPO) shows some selectivity for glial (IC50 = 268 mu M) versus neuronal (IC50 = 530 mu M) GABA uptake, exo-THPO (8) was shown to be more potent as an inhibitor of glial (IC50 = 200 mu M) rather than neuronal (IC50 = 900 mu M) GABA uptake. This selectivity was more pronounced for 9, which showed IC50 values of 40 and 500 mu M as an inhibitor of glial and neuronal GABA uptake, respectively. These effects of 8 and 9 proved to be enantioselective, (R)-(-)-8 and (R)-(+)-9 being the active inhibitors of both uptake systems. The selectivity of 9 as a glial GABA uptake inhibitor was largely lost by replacing the N-methyl group of 9 by an ethyl group, compound 10 being an almost equipotent inhibitor of glial (IC50 = 280 mu M) and neuronal (IC50 = 400 mu M) GABA uptake. The remaining target compounds, 11-17, were very weak or inactive as inhibitors of both uptake systems. Compounds 9-13 and 15 were shown to be essentially inactive against isoniazide-induced convulsions in mice after subcutaneous administration. The isomeric pivaloyloxymethyl derivatives of 9, compounds 43 and 44, were synthesized and tested as potential prodrugs in the isoniazide animal model. Both 43 (ED50 = 150 mu mol/kg) and 44 (ED50 = 220 mu mol/kg) showed anticonvulsant effects, and this effect of 43 was shown to reside in the (R)-(+)-enantiomer, 45 (ED50 = 44 mu mol/kg). Compound 9 also showed anticonvulsant activity when administered intracerebroventricularly (ED50 = 59 nmol).

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, 35963-20-3. The above is the message from the blog manager. COA of Formula: C10H16O4S.

Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Synthetic Route of 133-37-9, Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, 133-37-9, Name is (2R,3R)-rel-2,3-Dihydroxysuccinic acid, SMILES is O=C(O)[C@H](O)[C@@H](O)C(O)=O, belongs to Benzisoxazole compound. In a article, author is Cullen, William, introduce new discover of the category.

Catalysis in a Cationic Coordination Cage Using a Cavity-Bound Guest and Surface-Bound Anions: Inhibition, Activation, and Autocatalysis

The Kemp elimination (reaction of benzisoxazole with base to give 2-cyanophenolate) is catalyzed in the cavity of a cubic M8L12 coordination cage because of a combination of (i) benzisoxazole binding in the cage cavity driven by the hydrophobic effect, and (ii) accumulation of hydroxide ions around the 16+ cage surface driven by ion pairing. Here we show how reaction of the cavity-bound guest is modified by the presence of other anions which can also accumulate around the cage surface and displace hydroxide, inhibiting catalysis of the cage-based reaction. Addition of chloride or fluoride inhibits the reaction with hydroxide to the extent that a new autocatalytic pathway becomes apparent, resulting in a sigmoidal reaction profile. In this pathway the product 2-cyanophenolate itself accumulates around the cationic cage surface, acting as the base for the next reaction cycle. The affinity of different anions for the cage surface is therefore 2-cyanophenolate (generating autocatalysis) > chloride > fluoride (which both inhibit the reaction with hydroxide but cannot deprotonate the benzisoxazole guest) > hydroxide (default reaction pathway). The presence of this autocatalytic pathway demonstrates that a reaction of a cavity-bound guest can be induced with different anions around the cage surface in a controllable way; this was confirmed by adding different phenolates to the reaction, which accelerate the Kemp elimination to different extents depending on their basicity. This represents a significant step toward the goal of using the cage as a catalyst for bimolecular reactions between a cavity-bound guest and anions accumulated around the surface.

Synthetic Route of 133-37-9, Consequently, the presence of a catalyst will permit a system to reach equilibrium more quickly, but it has no effect on the position of the equilibrium as reflected in the value of its equilibrium constant.I hope my blog about 133-37-9 is helpful to your research.

Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Synthetic Route of 843666-40-0, Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. 843666-40-0, Name is 18-(tert-Butoxy)-18-oxooctadecanoic acid, SMILES is O=C(O)CCCCCCCCCCCCCCCCC(OC(C)(C)C)=O, belongs to Benzisoxazole compound. In a article, author is COHEN, LJ, introduce new discover of the category.

RISPERIDONE

Risperidone, a benzisoxazole derivative, is a novel antipsychotic agent that has an extremely strong binding affinity for serotonin 5-HT2 receptors, a strong binding affinity for dopamine D2 receptors, and a high affinity for alpha1- and alpha2-adrenergic receptors and histamine H-1 receptors. Its affinity for serotonin receptors is approximately 200 times greater than that of haloperidol, and its dopamine antagonistic potency is comparable to that of haloperidol. Its major metabolite, 9-hydroxyrisperidone, has similar pharmacologic activity, and thus the parent compound and metabolite form the active antipsychotic moiety Clinical trials demonstrate that risperidone is an effective antipsychotic agent that improves negative as well as positive symptoms of schizophrenia. At recommended dosages, the frequency of extrapyramidal side effects is no greater than that seen with placebo. The drug appears to be an advance in the treatment of psychoses.

Synthetic Route of 843666-40-0, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 843666-40-0.

Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. Recommanded Product: 3-(2-Amino-2-oxoethyl)-5-methylhexanoic acid, 181289-15-6, Name is 3-(2-Amino-2-oxoethyl)-5-methylhexanoic acid, SMILES is CC(C)CC(CC(N)=O)CC(O)=O, in an article , author is Nunes, Claudio M., once mentioned of 181289-15-6.

Heavy-Atom Tunneling Through Crossing Potential Energy Surfaces: Cyclization of a Triplet 2-Formylarylnitrene to a Singlet 2,1-Benzisoxazole

Not long ago, the occurrence of quantum mechanical tunneling (QMT) chemistry involving atoms heavier than hydrogen was considered unreasonable. Contributing to the shift of this paradigm, we present here the discovery of a new and distinct heavy-atom QMT reaction. Triplet syn-2-formyl-3-fluorophenylnitrene, generated in argon matrices by UV-irradiation of an azide precursor, was found to spontaneously cyclize to singlet 4-fluoro-2,1-benzisoxazole. Monitoring the transformation by IR spectroscopy, temperature-independent rate constants (k approximate to 1.4×10(-3) s(-1); half-life of approximate to 8 min) were measured from 10 to 20 K. Computational estimated rate constants are in fair agreement with experimental values, providing evidence for a mechanism involving heavy-atom QMT through crossing triplet to singlet potential energy surfaces. Moreover, the heavy-atom QMT takes place with considerable displacement of the oxygen atom, which establishes a new limit for the heavier atom involved in a QMT reaction in cryogenic matrices.

But sometimes, even after several years of basic chemistry education, it is not easy to form a clear picture on how they govern reactivity! 181289-15-6, you can contact me at any time and look forward to more communication. Recommanded Product: 3-(2-Amino-2-oxoethyl)-5-methylhexanoic acid.

Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics

Chemistry is an experimental science, Recommanded Product: 57-11-4, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 57-11-4, Name is Stearic acid, molecular formula is C18H36O2, belongs to Benzisoxazole compound. In a document, author is Okada, M.

Effects of zonisamide on dopaminergic system

Effects of zonisamide (ZNS) on extracellular dopamine (DA), its precursor 3,4-dihydroxyphenylalanine (DOPA), its metabolites 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) levels in the striatum as well as hippocampus of freely moving rats were studied. Intracellular DA, DOPA, DOPAC and HVA levels, as well as DOPA accumulation as an index of tyrosine hydroxylase activity in the rat brain in vivo, DA re-uptake in the striatum and hippocampus, and monoamine oxidase (MAO) activities were also determined. Acute administrations of therapeutic ZNS doses (20 and 50 mg/kg) increased striatal extracellular DOPA levels, intracellular striatal and hippocampal DOPA levels, and stimulated DOPA accumulation in both brain regions. ZNS also increased striatal and hippocampal intracellular as well as extracellular DA and MIA Levels, but decreased those of DOPAC levels. Chronic (3 weeks) administrations of therapeutic ZNS doses (20 and 50 mg/kg/day) increased intracellular DA, DOPA, DOPAC and HVA levels in striatum and hippocampus. ZNS-induced changes were greater in intracellular levels than in extracellular levels. Acute and chronic supratherapeutic ZNS dose (100 mg/kg) administration decreased intracellular levels of all substances detectable in both brain regions, and inhibited DOPA accumulation. Both subtypes of MAO (type A and type B) activities were weakly inhibited by ZNS. ZNS showed no effect on DA re-uptake in striatum nor in hippocampus. These results suggest that therapeutic ZNS doses increase DOPA accumulation as well as both intracellular and extracellular DA, DOPA and HVA levels. However, such doses also decrease extracellular and intracellular DOPAC levels by enhancing DA synthesis and/or by selectively inhibiting MAO-B activities. In addition, chronic therapeutic ZNS dose administration enhances DA synthesis, which results in increased intracellular DA, its precursor and its metabolites levels. On the other hand, both acute and chronic supratherapeutic ZNS dose administrations inhibit DA turnover. These ZNS effects on DA metabolism are at least partly involved in the mechanisms of action of ZNS.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law. In my other articles, you can also check out more blogs about 57-11-4. Recommanded Product: 57-11-4.

Reference:
Benzisoxazole – Wikipedia,
,Benzisoxazole – an overview | ScienceDirect Topics