Discovery of 1,2-Benzisoxazole-3-acetic Acid

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SYNTHESIS OF 4-OXO-4H-BENZISOXAZOLO<2,3-a>PYRIDINES VIA DIMERIZATION OF 1,2-BENZISOXAZOLE-3-ACETIC ACIDS

Reactions of 1,2-benzisoxazole-3-acetic acid (1) with tosyl chloride and acyl chlorides in pyridine afforded the corresponding 4-oxo-4H-benzisoxazolo<2,3-a>pyridines (2).KEYWORDS – 1,2-benzisoxazole-3-acetic acids; dimerization; mixed anhydrides; tosyl chloride; N-C bond formation; 4-oxo-4H-benzisoxazolo<2,3-a>pyridines

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Discovery of 1,2-Benzisoxazole-3-acetic Acid

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Process for the preparation of 1,2-benzisoxazole-3-acetic acid

The present invention provides a process for preparing 1,2-benzisoxazole-3-acetic acid, comprising the step of reacting 4-hydroxy-coumarin with hydroxyl-amine in the presence of a base. The present invention further provides a process for preparing a salt of benzisoxazole methane sulfonic acid, comprising the steps of 1) sulfonating 1,2-benzisoxazole-3-acetic acid using chlorosulfonic acid in a solvent mixture comprising methylene chloride and sodium hydroxide; and 2) isolating the salt of benzisoxazole methane sulfonic acid.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Discovery of 1,2-Benzisoxazole-3-acetic Acid

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Novel Base-induced Reactions of Substituted (1,2-Benzisoxazol-3-yl)acetates

The reactions of substituted (1,2-benzisoxazol-3-yl)acetates with strong bases are described.The esters (1) and (2) having electron-donating and dialkylamino substituents undergo novel ring transformations on treatment with NaH, ButOK, or MeONa in DMF to afford the 2H-azirines (8) and the 3-iminobenzofurans (18), respectively, while under similar conditions the halogeno esters (3) dimerize to give the ethylenedicarboxylate (24).Treatment of the esters (4)-(7) having electron-withdrawing substituents with NaH in DMF results in the recovery of the starting esters.However, on treatment of the sulphinyl esters (6) with MeONa in methanol, C-S bond cleavage occurs to afford methyl arylsulphinates (27).

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Extracurricular laboratory:new discovery of 1,2-Benzisoxazole-3-acetic Acid

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New Somatostatin receptor subtype 4 (SSTR4) agonists

3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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2-Cyclic amino-2-(1,2-benzisoxazol-3-yl)acetic acid ester derivatives, process for the preparation thereof and composition containing the same

Novel 2-cyclic amino-2-(1,2-benzisoxazol-3-yl)acetic acid derivatives of the formula: STR1 wherein R1 is hydrogen or a halogen atom, R2 is a lower alkyl group, Am is a 5- to 9-membered saturated cyclic amino group which may be substituted by a lower alkyl group, and the group: STR2 binds to the piperidine moiety at 3- or 4-position of the latter, and their pharmaceutically acceptable acid addition salts and quaternary ammonium salts, process for their preparation, and pharmaceutical compositions containing these compounds. They have potent anticholinergic antispasmodic activity, while they are weak in side effects such as mydriasis, inhibition of salivary secretion and tachycardia.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Awesome Chemistry Experiments For 1,2-Benzisoxazole-3-acetic Acid

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Process for the preparation of zonisamide and the intermediates thereof

The present invention provides a novel and improved process for the preparation of Zonisamide and the intermediates thereof. In one aspect of the present invention, the process provides for: the preparation and isolation of a novel crystalline form of anhydrous 1,2-benzisoxazole-3-methanesulfonic acid of formula 1; the direct chlorination of the acid of formula 1 into its acid chloride of formula 2; and the in situ conversion of the intermediate acid chloride of formula 2 into Zonisamide.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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An amino-sulfonyl compound, a process for their preparation and use (by machine translation)

Disclosed are an aminosulfonyl compound represented by general formula I or a tautomer, enantiomer, racemate or pharmaceutically acceptable salt thereof, a preparation method therefor, a pharmaceutical composition and a use thereof. The compound can be used for treating epilepsy, convulsion, obesity and the like.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Conventional & non conventional synthesis of biologically active novel pyrimidine and its moleculer descriptor study

3-Formylchromones 1 when treated with 2-(benzo[cf]isoxazol-3-yl) acetic acid 2 under microwave irradiation afforded 3-((E)-2-benzo[c/] isoxazol-3-yl) vinyl)-4H-chromen- 4-ones (3). Compounds 3 on treatment with thiourea gave the compound 5-(2- (benzo[d]isoxazol-3-yl) vinyl)-4(-2-hydroxypenyl) pyrimidine-2(1H)- Thiones 4. Compounds 3 on treatment with guanidine gave the compound 2-(5-(2- (benzol[dJisoxazol-3-yl)vinyl)-l,2-dihydro-2-iminopyrimidin-4- yl) phenols 5. Moleculer descriptor properties were analyzed by using simple moleculer descriptor used by “Lipinski’s rule of 5”. The structures of compounds were established on the basis of spectral data. Synthesized compounds were screened for their antimicrobial activities.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Synthesis and biological activity of a series of aryl tropanyl esters and amides chemically related to 1H-indole-3-carboxylic acid endo 8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester. Development of a 5-HT4 agonist endowed with potent antinociceptive activity

A series of aryl tropanyl esters and amides related to 1H-indole-3-carboxylic acid endo 8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester (ICS 205930, CAS 89565-68-4) were synthesized and evaluated for antinociceptive activity using the hot-plate test. Of these, the benzofurane-3-carboxylic ester of tropine (1) was found powerfully to increase the pain threshold, with a cholinergic mechanism of action. Despite the structural similarity with ICS 205930, the analgesia induced by 1 seems not to be due to 5-HT3 receptor interaction, and there is evidence of involvement of the central 5-HT4 receptor.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

The important role of 4865-84-3

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Targeting of Fumarate Hydratase from Mycobacterium tuberculosis Using Allosteric Inhibitors with a Dimeric-Binding Mode

With the growing worldwide prevalence of antibiotic-resistant strains of tuberculosis (TB), new targets are urgently required for the development of treatments with novel modes of action. Fumarate hydratase (fumarase), a vulnerable component of the citric acid cycle in Mycobacterium tuberculosis (Mtb), is a metabolic target that could satisfy this unmet demand. A key challenge in the targeting of Mtb fumarase is its similarity to the human homolog, which shares an identical active site. A potential solution to this selectivity problem was previously found in a high-throughput screening hit that binds in a nonconserved allosteric site. In this work, a structure-activity relationship study was carried out with the determination of further structural biology on the lead series, affording derivatives with sub-micromolar inhibition. Further, the screening of this series against Mtb in vitro identified compounds with potent minimum inhibitory concentrations.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics