Category: 868-14-4

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, 868-14-4, Name is Potassium hydrogen tartrate, SMILES is [O-]C(C(C(C(O)=O)O)O)=O.[K+], belongs to Benzisoxazole compound. In a document, author is Zhang, Donglu, introduce the new discover, COA of Formula: C4H5KO6.

Reductive isoxazole ring opening of the anticoagulant razaxaban is the major metabolic clearance pathway in rats and dogs

Razaxaban is a selective, potent, and orally bioavailable inhibitor of coagulation factor Xa. The molecule contains a 1,2-benzisoxazole structure. After oral administration of [C-14] razaxaban to intact and bile duct-cannulated rats (300 mg/kg) and dogs (20 mg/kg), metabolism followed by biliary excretion was the major elimination pathway in both species, accounting for 34 to 44% of the dose, whereas urinary excretion accounted for 3 to 13% of the dose. Chromatographic separation of radioactivity in urine, bile, and feces of rats and dogs showed that razaxaban was extensively metabolized in both species. Metabolites were identified on the basis of liquid chromatography/tandem mass spectrometry and comparison with synthetic standards. Among the 12 metabolites identified, formation of an isoxazole-ring opened benzamidine metabolite (M1) represented a major metabolic pathway of razaxaban in rats and dogs. However, razaxaban was the major circulating drug-related component (>70%) in both species, and M1, M4, and M7 were minor circulating components. In addition to the in vivo observations, M1 was formed as the primary metabolite in rat and dog hepatocytes and in the rat liver cytosolic fraction. The formation of M1 in the rat liver fraction required the presence of NADH. Theses results suggest that isoxazole ring reduction, forming a stable benzamidine metabolite (M1), represents the primary metabolic pathway of razaxaban in vivo and in vitro. The reduction reaction was catalyzed by NADH-dependent reductase(s) in the liver and possibly by intestinal microflora on the basis of the recovery of M1 in feces of bile duct-cannulated rats.

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 868-14-4 is helpful to your research. COA of Formula: C4H5KO6.

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. 868-14-4, Name is Potassium hydrogen tartrate, molecular formula is C4H5KO6, belongs to Benzisoxazole compound, is a common compound. In a patnet, author is Soeiro, Pedro F., once mentioned the new application about 868-14-4, Computed Properties of C4H5KO6.

The Synthesis of 2-Spiroindolin-3-one-(thio)barbiturates from 2,1-Benzisoxazoles: A Rearrangement Promoted by Thermal Conditions

A new thermal process to prepare spiroindolin-3-ones from 3-substituted 2,1-benzisoxazoles in good yields (70-85%) is described. The highest yields were observed when microwave irradiation was used. The method does not require the use of any additive or catalyst. A possible reaction mechanism involving a nitrene key intermediate is proposed.

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, 868-14-4. The above is the message from the blog manager. Computed Properties of C4H5KO6.

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

Electric Literature of 868-14-4, Redox catalysis has been broadly utilized in electrochemical synthesis due to its kinetic advantages over direct electrolysis. The appropriate choice of redox mediator can avoid electrode passivation and overpotential. 868-14-4, Name is Potassium hydrogen tartrate, SMILES is [O-]C(C(C(C(O)=O)O)O)=O.[K+], belongs to Benzisoxazole compound. In a article, author is Safaei-Ghomi, Javad, introduce new discover of the category.

A convenient method for the preparation of 2-aminobenzophenone derivatives under ultrasonic irradiation

A quick and convenient method for the preparation of 2-aminobenzophenone derivatives is described. This approach consists of the nucleophilic substitution reaction of nitrobenzenes by phenylacetonitrile under conventional and ultrasonic conditions followed by reduction of the produced 2,1-benzisoxazole to 2-aminobenzophenone. This 2-step reaction was studied by changing the reaction parameters (reaction temperature, ultrasound power, and reaction time). The results clearly demonstrated that using ultrasound irradiation results in a high yield within a short reaction time.

Electric Literature of 868-14-4, 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 868-14-4.

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

Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 868-14-4, Name is Potassium hydrogen tartrate, molecular formula is C4H5KO6, belongs to Benzisoxazole compound. In a document, author is Weyland, M., introduce the new discover, Application In Synthesis of Potassium hydrogen tartrate.

Artificial enzymes based on imprinted liquid-crystalline materials

Liquid-crystal elastomers, imprinted around indole, are assessed as artificial enzymes for the isomerisation of benzisoxazole into 2-cyano phenol. Two types of material are synthesised, tested in the catalysis and compared with non-liquid-crystal imprinted polymers: an imprinted liquid-crystalline elastomer and a semi-interpenetrated imprinted liquid-crystal network. The catalytic effect of all materials is close. However, the main benefit for the liquid-crystal elastomer is shown to be the shape memory of the material at the molecular scale, because the isomerisation kinetics are found to be identical before and after deformation of the cavities either by thermal treatment up to the isotropic state or by solvent induced swelling. This fact is related to the coupling between the order and the conformation of the polymer chains, which is fixed by the crosslinking process. On the other hand, the imprinted sites of the semi-interpenetrated imprinted liquid-crystal elastomer are shown to be almost 100 times more active than the non-imprinted sites in the catalysis. This factor is only 22 for the corresponding non-liquid-crystalline network.

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 868-14-4. Application In Synthesis of Potassium hydrogen tartrate.

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. 868-14-4, Name is Potassium hydrogen tartrate, molecular formula is C4H5KO6, belongs to Benzisoxazole compound, is a common compound. In a patnet, author is Crabtree, Brian L., once mentioned the new application about 868-14-4, Recommanded Product: 868-14-4.

Iloperidone for the Management of Adults with Schizophrenia

Background: Iloperidone is a second-generation antipsychotic drug approved in May 2009 by the US Food and Drug Administration (FDA) for the acute treatment of schizophrenia in adults. It is a piperidinyl-benzisoxazole derivative with mixed serotonin (5HT2A) and D2 dopamine antagonist properties. Objective: The purpose of this article was to review the pharmacology, pharmacokinetics, efficacy, safety, and role in treatment for iloperidone in schizophrenia. Methods: Scientific and clinical data were collected through searches of PubMed, ClinicalTrials.gov, International Pharmaceutical Abstracts, and the FDA, using the search term iloperidone, and limited to English-language articles. Reference lists were reviewed for additional publications. Dates included the beginning of the database through 2010. No limits were placed on study design. Results: In a 4-week Phase III trial, iloperidone 12 mg twice daily lowered the Positive and Negative Syndrome Scale (PANSS) total scores to a significantly greater extent than did placebo (-12 vs -7.1; P < 0.01). The ziprasidone active control also separated from placebo (-12.3 vs -7.1; P < 0.05). A pooled analysis of 3 Phase III trials compared iloperidone in divided doses to placebo. The primary outcome was reduction in PANSS scores. Study 1 included iloperidone 4, 8, or 12 mg/d, haloperidol as an active control, and placebo. The PANSS reduction in the 12 mg/d group was significantly greater at end point versus baseline when compared with placebo (-9.9 vs -4.6; P = 0.047). Study 2 included iloperidone 4 to 8 mg/d or 10 to 16 mg/d, risperidone 4 to 8 mg/d, or placebo. The primary efficacy measure was change from baseline to end point in the Brief Psychiatric Rating Scale (BPRS). Improvement from baseline on all iloperidone doses was significantly greater than with placebo (4-8 mg/d group: -6.2, P = 0.012; 10-16 mg/d group: -7.2, P = 0.001; placebo, -2.5). Study 3 included iloperidone 12 to 16 mg/d, risperidone 6 to 8 mg/d, and placebo. The results on the primary efficacy variable, reduction in the BPRS score, was not significant for the 12 to 16 mg/d group versus placebo (-7.1 vs -5.0; P = 0.09), but was significant for the 20 to 24 mg/d iloperidone group (-8.6 vs -5.0; P = 0.01) and for the risperidone group (-11.5 vs 5.0; P < 0.001). A 52-week maintenance trial included iloperidone versus haloperidol as an active control. The primary efficacy variable was time to relapse. Comparison of mean time to relapse of the 2 arms showed no significant difference. The most common adverse events (AEs) associated with iloperidone were dizziness (5.1%-23.2%), dry mouth (5.2%-10.4%), somnolence (4%-13%), and dyspepsia (4.8%-7.8%). AEs appeared dose related. Prescribing information recommends a starting dosage of 1 mg twice daily and then titrated over 7 days to reach a target dosage of 12 to 24 mg/d. The titration is necessary to reduce the risk of orthostatic hypotension-related dizziness. Conclusions: Data support that when titrated slowly to a therapeutic dosage, iloperidone is generally well tolerated, has a favorable safety profile, and is an effective treatment option in patients with schizophrenia. Its place in therapy and performance in a typical patient population remain to be established. Slow initial titration and twice-daily dosing are potential disadvantages. (Clin Ther. 2011;33:330-345) (C) 2011 Published by Elsevier HS Journals, Inc. We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, 868-14-4. The above is the message from the blog manager. Recommanded Product: 868-14-4.

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

Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 868-14-4, Name is Potassium hydrogen tartrate, molecular formula is C4H5KO6, belongs to Benzisoxazole compound. In a document, author is Naumov, P, introduce the new discover, Product Details of 868-14-4.

Latent photochromism (pseudothermochromism) and photofatigue of crystalline 2-(2 ‘,4 ‘-dinitrobenzyl)pyridine

Along with the metastable 2-(2,4′-dinitrophenylmethylidene)-1,2-dihydropyridine (NH) and the unstable 6-aci-nitro-2-nitro-5-(2-pyridylmethylene)-1,3-cyclohexadiene (OH), the stable form of 2-(2′,4′-dinitrobenzyl)pyridine (DNBP), CH, is photochemically converted into small amounts of 1,2-bis(2′,4-dinitrophenyl)-1,2-bis(2′-pyridyl)ethane, trans-bis[5-nitro-2-(pyridine-2-carbonyl)phenyl]diazene N-oxide, 6-nitro-3-(2’-pyridyl)-2,1-benzisoxazole and 3-nitropyrido[1,2-b]quinolin-6-ium-11-olate. The latent photochromism of DNBP, as shown by x-ray analysis of the structures of the side-products and ESR/IR measurements, is attributed to open-shell reactions that are initiated by hydrogen photoabstraction and subsequent creation of two monoradicals, NH. and OH.. Large amounts of the radicals (ca 50% NH. and 70% OH) confined in the crystalline interior are persistent under ambient conditions. Through quasi-periodic reactions, the remaining radicals partially recover the ground-state isomers CH, NH and OH, or decay to the side-products, which results in crystalline photofatigue. Together with proton tunneling from the excited CH, the radical reactions represent dominant mechanism for the creation of NH and OH in the low-temperature regimes, but are successfully competed by the closed-shell reactions at higher temperatures. The precursor state, whose existence was assumed previously from transient absorption spectroscopy, may be identified as the radical OH.. The present work represents the first study of the photofatigue of a 2-(2,4-dinitrobenzyl)pyridine compound and extends the ‘classical’ mechanism of the photochromic reactions of nitrobenzylpyridines with a set of open-shell radical reaction routes. Copyright (C) 2004 John Wiley Sons, Ltd.

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 868-14-4. Product Details of 868-14-4.

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

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 868-14-4, Name is Potassium hydrogen tartrate, molecular formula is C4H5KO6. In an article, author is Brown-Proctor, C,once mentioned of 868-14-4, Category: Benzisoxazole.

Synthesis and evaluation of 6-[C-11]methoxy-3-[2-[l-(phenylmethyl)-4-piperidinyl]ethyl]-1,2-benzisoxazole as an in vivo radioligand for acetylcholinesterase

6-Methoxy-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-1,2-benzisoxazole is a high affinity (K-i = 8.2 nM) reversible inhibitor of acetylcholinesterase (AChE). The carbon-11 labeled form was prepared in high (>97%) radiochemical purity and with specific activities of 37 +/- 20 GBq/mu mol at end of synthesis, by the alkylation of the desmethyl precursor with [C-11]methyl trifluoromethanesulfonate in N,N dimethylformamide at room temperature. In vivo studies in mice demonstrated good blood brain permeability but essentially uniform regional brain distribution. Thus, despite in vitro and in vivo activity as an AChE inhibitor, 6-[C-11]methoxy-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-1,2-benzisoxazole does not appear to be a good candidate for in vivo imaging studies of AChE in the mammalian brain. NUCL MED BIOL 26;1: 99-103, 1999. (C) 1999 Elsevier Science Inc.

Interested yet? Keep reading other articles of 868-14-4, you can contact me at any time and look forward to more communication. Category: Benzisoxazole.

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

Chemistry, like all the natural sciences, HPLC of Formula: C4H5KO6, begins with the direct observation of nature¡ª in this case, of matter.868-14-4, Name is Potassium hydrogen tartrate, SMILES is [O-]C(C(C(C(O)=O)O)O)=O.[K+], belongs to Benzisoxazole compound. In a document, author is Vijayakumar, E. K. S., introduce the new discover.

HPLC method for simultaneous determination of impurities and degradation products in zonisamide

A gradient reversed phase HPLC method was developed and validated for the analysis of related substances in zonisamide (1,2-benzisoxazole-3-methanesulfonamide), using a Waters Symmetry C8 (150FNx013.9 mm) column with a flow rate of 1.0 ml/min and detection at 280 nm. The mobile phase component A consisted of a mixture of 0.02 M aqueous potassium dihydrogen phosphate-acetonitrile-methanol (75:10:15 v/v/v), pH adjusted to 4.0 with orthophosphoric acid. The mobile phase component B consisted of a mixture of 0.02 M aqueous potassium dihydrogen phosphate-acetonitrile-methanol (15:40:45 v/v/v), pH 2.0 with orthophosphoric acid. The limit of detection and limit of quantitation were in the range of 0.001-0.007 and 0.0035-0.25 respectively with respect to sample concentration of 2 mg/ml. The method was linear in the range of LOQ level to 200 of specified limits for II-VIII (< 0.10, r (2) = 0.9958-0.9999). The method is sensitive, specific, linear, accurate, precise and stability-indicating for the detection and quantitation of precursors (viz., 4-hydroxycoumarin, 1,2-benzisoxazole-3-acetic acid, 1,2-benzisoxazole-3-bromoacetic acid, 1,2-benzisoxazole-3-methylbromide, sodium 1,2-benzisoxazole-3-methanesulfonate), process impurities (viz., 2-hydroxyacetophenone oxime and 3,3,3-tribromomethyl-1,2-benzisoxazole) and drug degradation products formed under stress conditions. 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. you can also check out more blogs about 868-14-4. HPLC of Formula: C4H5KO6.

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.868-14-4, Name is Potassium hydrogen tartrate, SMILES is [O-]C(C(C(C(O)=O)O)O)=O.[K+], belongs to Benzisoxazole compound. In a document, author is Sudharsana, S., introduce the new discover, SDS of cas: 868-14-4.

Molecular docking and simulation studies of 3-(1-chloropiperidin-4-yl)-6-fluoro benzisoxazole 2 against VP26 and VP28 proteins of white spot syndrome virus

White spot syndrome virus (WSSV), an aquatic virus infecting shrimps and other crustaceans, is widely distributed in Asian subcontinents including India. The infection has led to a serious economic loss in shrimp farming. The WSSV genome is approximately 300 kb and codes for several proteins mediating the infection. The envelope proteins VP26 and VP28 play a major role in infection process and also in the interaction with the host cells. A comprehensive study on the viral proteins leading to the development of safe and potent antiviral therapeutic is of adverse need. The novel synthesized compound 3-(1-chloropiperidin-4-yl)-6-fluoro benzisoxazole 2 is proved to have potent antiviral activity against WSSV. The compound antiviral activity is validated in freshwater crabs (Paratelphusa hydrodomous). An in silico molecular docking and simulation analysis of the envelope proteins VP26 and VP28 with the ligand 3-(1-chloropiperidin-4-yl)-6-fluoro benzisoxazole 2 are carried out. The docking analysis reveals that the polar amino acids in the pore region of the envelope proteins were involved in the ligand binding. The influence of the ligand binding on the proteins is validated by the molecular dynamics and simulation study. These in silico approaches together demonstrate the ligand’s efficiency in preventing the trimers from exhibiting their physiological function.

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 868-14-4 is helpful to your research. SDS of cas: 868-14-4.

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

Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. , COA of Formula: C4H5KO6, 868-14-4, Name is Potassium hydrogen tartrate, molecular formula is C4H5KO6, belongs to Benzisoxazole compound. In a document, author is Caccia, S, introduce the new discover.

Biotransformation of post-clozapine antipsychotics – Pharmacological implications

The need to develop new antipsychotics that have fewer motor adverse effects and offer better treatment of negative symptoms has led to a new generation of drugs. Most of these drugs undergo extensive first-pass metabolism and are cleared almost exclusively by metabolism, except for amisulpride whose clearance is largely due to urinary excretion. Risperidone has metabolic routes in common with ziprasidone but shows differences in regard to other main pathways: the benzisoxazole moiety of risperidone is oxidised by cytochrome P450 (CYP) 2D6 to the active 9-hydroxyrisperidone, whereas the benzisothiazole of ziprasidone is primarily oxidised by CYP3A4, yielding sulfoxide and sulfone derivatives with low affinity for target receptors in vitro. Olanzapine, quetiapine and zotepine also have some common metabolic features. However, for the thienobenzodiazepine olanzapine a main metabolic route is direct conjugation at the benzodiazepine nucleus, whereas for the dibenzothiazepine quetiapine and the dibenzothiepine zotepine iris CYP3A4-mediated oxidation, leading to sulfoxidation, hydroxylation and dealkylation for quetiapine, but N-demethylation to the active nor-derivative for zotepine. Although the promising benzisoxazole (iloperidone) and benzisothiazole (perospirone) antipsychotics share some metabolic routes with the structurally related available drugs, they too have pharmacologically relevant compound-specific pathways. For some of the new antipsychotics we know the isoenzymes involved in their main metabolic pathways and the endogenous and exogenous factors that, by affecting enzyme activity, can potentially modify steady-state concentrations of the parent drug or its metabolite(s), but we know very little about others (e.g. amisulpride isomers, nemonapride). For yet others, information is scarce about the activity of the main metabolites and whether and how these contribute to the effect of the parent drug. Aging reduces the clearance of most antipsychotics, except amisulpride (which requires further evaluation) and ziprasidone. Liver impairment has little or no effect on the pharmacokinetics of olanzapine, quetiapine, risperidone (and 9-hydroxy-risperidone) and ziprasidone, but information is lacking for amisulpride. Renal impairment significantly reduces the clearance and prolongs the elimination half-life of amisulpride and risperidone. Again, studies are still not available for some drugs (zotepine) and have focused on the parent drug for others (olanzapine, quetiapine, ziprasidone) despite the fact that renal impairment would be expected to lower the clearance of more polar metabolites. Addressing these issues may assist clinicians in the design of safe and effective regimens for this group of drugs, and in selecting the best agent for each specific population.

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 868-14-4. COA of Formula: C4H5KO6.

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