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A new process for the preparation of 1,2-benzisoxazole-3-methanesulfonates and 4-oximino-2,3dihydrobenzoxathiin- 2,2-dioxides (sultone oximes) is described. These compounds are important intermediates for the preparation of zonisamide, an anti-convulsant drug.

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Benzisoxazole – Wikipedia,
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An efficient and convenient methodology has been developed for the conversion of 2-hydroxy phenyl ketoxime to 1,2-benzisoxazole 2-oxide with sodium perborate (SPB) in glacial acetic acid under mild reaction conditions. Interestingly when the reaction was carried out under reflux condition deoximation was observed in quantitative yield.

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Risperidone is a benzisoxazole derivative which has proven efficacy against the positive and negative symptoms of schizophrenia It has mon recently been investigated and shown efficacy as a treatment for the behavioural and psychological symptoms associated with dementia in the elderly. Risperidone has pharmacological properties resembling those of the atypical antipsychotic clozapine and an improved tolerability profile compared with the conventional antipsychotic haloperidol. Risperidone has antagonistic activity primarily at serotonin 5-HT2A and dopamine D-2 receptors. In the first 2 large, well controlled trials of an antipsychotic agent used in the treatment of elderly patients with Alzheimer’s dementia, vascular dementia or mixed demential risperidone 1 mg/day was at least as effective as haloperidol and superior to placebo. as assessed by the rating scales for global behaviour, aggression and psychosis. In extension phases of the 2 trials, clinical benefits were maintained for treatment periods of up to 1 year, with an incidence rate of tardive dyskinesia (2.6%) one-tenth of that seen with conventional antipsychotics. Risperidone, administered at a low dosage of 1 mg/day was associated with fewer extrapyramidal symptoms compared with haloperidol in elderly patients, Risperidone was well tolerated with no clinically relevant abnormalities in laboratory tests. vital signs or electrocardiogram results. Conclusion: The efficacy of risperidone has been demonstrated in the treatment of the behavioural and psychological symptoms associated with dementia in the elderly. Preliminary results from 1-year extension studies confirm the favourable efficacy and tolerability profile of risperidone 1 mg/day, Although head to head studies with other atypical antipsychotic agents are required and the long term use of the drug requires clarification, risperidone represents a generally well tolerated and effective treatment in the management of dementia-associated behavioural and psychological symptoms in the elderly.

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Benzisoxazole – Wikipedia,
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Decrypt The Mystery Of ((1R,4S)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonic acid

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The inhibitory effect of 3-hydroxy-4-amino-4,5,6,7-tetrahydro1,2-benzisoxazole (exo-THPO) and its N-methylated (N-methylexo-THPO) and N-ethylated (N-ethyl-exo-THPO) analogs, derived from gamma-aminobutyric acid (GABA) and 4,5,6,7-tetrahydroisoxazolo[4,5-c]pyridin-3-ol (THPO) on GABA transport was investigated using cultured neocortical neurons (GABAergic) and astrocytes and cloned mouse GABA transporters GAT1-4 expressed in human embryonic kidney (HEK) 293 cells. Anticonvulsant activity was assessed after i.c.v. administration to Frings audiogenic seizure-susceptible mice. Anticonvulsant activity of the O-pivaloyloxymethyl prodrug of N-methyl-exo-THPO was assessed after i.p. administration. Results from these studies were compared with those obtained from similar studies with the novel anticonvulsant drug tiagabine, which acts via inhibition of GABA transport. exo-THPO and its N-alkyl analogs inhibited neuronal, astrocytic, and GAT1-mediated GABA transport but not GABA uptake mediated by GAT2-4. N-Methyl-exo-THPO was 8-fold more potent as an inhibitor of astrocytic versus neuronal GABA uptake. The IC50 value for inhibition of GABA uptake by GAT1 closely reflected its IC50 value for inhibition of neuronal uptake. Tiagabine was approximately 1000-fold more potent than exoTHPO and its alkyl derivatives as an inhibitor of GABA uptake in cultured neural cells and GAT1-expressing HEK 293 cells. exoTHPO, its alkylated analogs, and tiagabine displayed a time- and dose-dependent inhibition of audiogenic seizures after i.c.v. administration. N-Methyl-exo-THPO was the most potent anticonvulsant among the exo-THPO compounds tested and only slightly less potent than tiagabine. The findings suggest a correlation between anticonvulsant efficacy and selective inhibition of astroglial GABA uptake. Furthermore, results obtained with the N-methyl-exo-THPO prodrug demonstrate the feasibility of developing a glial-selective GABA uptake inhibitor with systemic bioavailability.

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The mechanisms by which specific solvent properties influence the title reaction, which is extremely medium-sensitive, have been investigated using multiparametric methods. The results of this analysis have been compared with previous experimental studies of the reaction mechanism. Hydrogen-bond donation by solvent and hydrogen-bond donation by tetramethylguanidinium ion in tight ion pairs with the carboxylate greatly retard the reaction. Solvent dipolarity and basicity accelerate the reaction, most likely by helping to break up hydrogen-bonded ion pairs. The rate of decarboxylation in the binding pocket of a catalytic antibody developed for this reaction is slower than that expected of a free carboxylate in an aprotic environment. Therefore, the binding site may contain a hydrogen-bond-donating species. A better catalyst might be developed by approaches that reduce hydrogen bonding in the active site without reducing substrate binding.

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Benzisoxazole-3-acetic acid, a new synthetic growth regulator, was administered to protoplast cultures from Nicotiana tabacum and subsequently to the developed microcalluses, to test its activity on plant regeneration from protoplasts in different culture conditions. Such activity, compared to that of naphthalene-acetic acid, proved to be rather low in the stage of cellular division and microcallus formation but particulary high in the stage of shoot induction from microcallus, thus confirming that the activity of this compound is mainly morphogenetic.

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Introduction: Zonisamide is a benzisoxazole with 3-methanesulfonamide side chain, chemically unrelated with other anticonvulsants, and approved as mono-therapy of newly diagnosed focal epilepsy with or without secondary generalization in adults or adjunctive therapy in the treatment of partial seizures, with or without secondary generalization, in adults, adolescents, and children aged 6 years and above. Areas covered: Pharmacokinetics, clinical efficacy, and the adverse effects of zonisamide are discussed in the article. The discussion is based on data from published preclinical studies, clinical trials, observational studies, systematic reviews, and approved summary of product characteristics. Expert opinion: Zonisamide is an anticonvulsant with multiple mechanisms of action on neuronal tissue, which achieves seizure freedom in more than 80% of patients with newly-onset focal epilepsy and in 6.2 to 18.1% of patients with focal onset seizures inadequately controlled by first-line anticonvulsants. Within the recommended dose range, it follows linear kinetic of elimination; it is metabolized in the liver by two cytochrome isoforms, so pharmacokinetic interactions are rare and with little clinical significance. Up to 10% of patients taking zonisamide will have problems with weight loss and more than 10% with irritability, confusion or depression, and long-lasting therapy may cause renal calculi in 1.2% of patients.

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New Advances in Chemical Research in 2021. Chemistry is a science major with cience and engineering. The main research directions are chemical synthesis, and research on the structure and performance of functional materials. 35963-20-3, Name is ((1R,4S)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonic acid, SMILES is O=S(C[C@]1(C2(C)C)C(C[C@]2([H])CC1)=O)(O)=O, in an article , author is SATO, H, once mentioned of 35963-20-3, HPLC of Formula: https://www.ambeed.com/products/35963-20-3.html.

A practical procedure for synthesis of a new uricosuric agent, 5-chloro-7,8-dihydro-3-phenylfuro[2,3-g]-1,2-benzisoxazole-7-carboxylic acid (1, AA-193) is described, which starts from 2,5-dichlorophenol (3b) and involves 5-chloro-6-hydroxy-3-phenyl-1,2-benzisoxazole (2) as the key intermediate. Successive treatment of 3b with benzoyl chloride-aluminum chloride (AlCl3) and hot ethanolic sodium hydroxide gives 4-benzoyl-2,5-dichlorophenol (8, 61%), which is oximated with hydroxylamine hydrochloride and then transformed into the benzisoxazole 2 (88%) with potassium hydroxide in N,N-dimethylformamide (DMF) (method C). The reaction of 2 with aqueous formaldehyde and dimethylamine affords the Mannich base Ila (97%), which is treated with a sulfonium ylide 12, 14 or 15 followed by heating with sodium hydroxide (NaOH) in ethanol (EtOH) to give 1 in high yield (method E).

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Electric Literature of 35963-20-3, New discoveries in chemical research and development in 2021. 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. 35963-20-3, Name is ((1R,4S)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonic acid, SMILES is O=S(C[C@]1(C2(C)C)C(C[C@]2([H])CC1)=O)(O)=O, belongs to benzisoxazole compound. In a article, author is Jankovic, Slobodan M., introduce new discover of the category.

Introduction: Zonisamide is a benzisoxazole with 3-methanesulfonamide side chain, chemically unrelated with other anticonvulsants, and approved as mono-therapy of newly diagnosed focal epilepsy with or without secondary generalization in adults or adjunctive therapy in the treatment of partial seizures, with or without secondary generalization, in adults, adolescents, and children aged 6 years and above. Areas covered: Pharmacokinetics, clinical efficacy, and the adverse effects of zonisamide are discussed in the article. The discussion is based on data from published preclinical studies, clinical trials, observational studies, systematic reviews, and approved summary of product characteristics. Expert opinion: Zonisamide is an anticonvulsant with multiple mechanisms of action on neuronal tissue, which achieves seizure freedom in more than 80% of patients with newly-onset focal epilepsy and in 6.2 to 18.1% of patients with focal onset seizures inadequately controlled by first-line anticonvulsants. Within the recommended dose range, it follows linear kinetic of elimination; it is metabolized in the liver by two cytochrome isoforms, so pharmacokinetic interactions are rare and with little clinical significance. Up to 10% of patients taking zonisamide will have problems with weight loss and more than 10% with irritability, confusion or depression, and long-lasting therapy may cause renal calculi in 1.2% of patients.

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Benzisoxazole – Wikipedia,
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An efficient and convenient methodology has been developed for the conversion of 2-hydroxy phenyl ketoxime to 1,2-benzisoxazole 2-oxide with sodium perborate (SPB) in glacial acetic acid under mild reaction conditions. Interestingly when the reaction was carried out under reflux condition deoximation was observed in quantitative yield.

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Benzisoxazole – Wikipedia,
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